Abstract: The present invention provides drug conjugates comprising 5-aminolevulinic acid (ALA), an aldehyde and a carboxylic acid that may function as a histone deacetylase inhibitor (HDACI). These conjugates may serve as co-drugs which release a plurality of active species in vivo. The novel drug conjugates may be used, for the treatment or prevention of cancer in PDT-dependent and/or PDT-independent (nonPDT) treatments, as well as for cosmetic uses. In addition the present invention provides novel uses for both the novel and known compounds. According to some embodiments, the present invention provides drug conjugates (co-drugs) comprising (i) ALA, (ii) an aldehyde and (iii) a carboxylic acid that may function as a histone deacetylase inhibitor (HDACO for the treatment of anemia and/or for the induction of erythropoiesis.

Abstract: Provided is an enhancer for cancer thermotherapy not combined with photodynamic therapy. Cancer treatment not combined with photodynamic therapy is made available by using, as an enhancer for cancer thermotherapy, 5-aminolevulinic acids represented by formula (1): R2R1NCH2COCH2CH2COR3??(1) [wherein R1 and R2 each independently represent a hydrogen atom, an alkyl group, an acyl group, an alkoxycarbonyl group, an aryl group, or an aralkyl group; and R3 represents a hydroxy group, an alkoxy group, an acyloxy group, an alkoxycarbonyloxy group, an aryloxy group, an aralkyloxy group, or an amino group] or a salt thereof.

Abstract: The present disclosure provides antimicrobial compounds, compositions comprising such antimicrobial compounds, and methods of their use, in particular, antibacterial compounds and antifungal compounds. In certain aspects, the antimicrobial compounds are effective against pathogens of hospital-acquired infections. In certain aspects, the antimicrobial compounds are effective against pathogens that are resistant to antibiotics. The antimicrobial compounds can be used in antibacterial compositions, antifungal compositions, antiseptic compositions and disinfectant compositions. The antimicrobial compounds can be used as adjuncts in antibacterial compositions and antifungal compositions.

Abstract: The present invention provides novel Ruthenium-based transition metal complex catalysts comprising specific ligands, their preparation and their use in hydrogenation processes. Such complex catalysts are inexpensive, thermally robust, and olefin selective.

Abstract: Disclosed herein are novel cationic lipids that can be used in combination with other lipid components such as cholesterol and PEG-lipids to form lipid nanoparticles with oligonucleotides. The cationic lipids can demonstrate enhanced efficacy along with lower liver toxicity as a result of lower lipid levels in the liver. The present invention employs low molecular weight cationic lipids with one short lipid chain coupled with inclusion of hydrolysable functionality in the lipid chains to enhance the efficiency and tolerability of in vivo delivery of siRNA.

Abstract: A first aspect of the invention is a compound (sometimes also referred to herein as an “active agent” or “active compound”) of Formula I or Ia: or a pharmaceutically acceptable salt or prodrug thereof. Compositions thereof and methods of using the same (e.g. for the treatment of a neurological disease) are also described.

Abstract: The present invention relates to novel 3,5-bis(fluoroalkyl)pyrazole-4-carboxylic acid derivatives and to a process for preparing 3,5-bis(fluoroalkyl)pyrazole-4-carboxylic acid derivatives and 3,5-bis(fluoroalkyl)pyrazoles.

Abstract: This invention relates to a novel crystalline polymorph of hexyl-5-aminolevulinate hydrochloride, referred to hereinafter as Form C, which is useful as precursor of a photo sensitizer in the photodynamic diagnosis and treatment of metabolically active cells related to diseases such as cancer of the uterus, cervix, vagina, rectum, colon, lower gastrointestinal tract; infection associated with cancer caused by human papilloma virus; non-cancerous lower gastrointestinal tract a human; inflammatory bowel disease; ulcerative colitis; Crohn's disease; inflammatory bowel syndrome; dysplasia of the female reproductive system; anus; penis; rosacea; and acne and which is suitable for use as the active ingredient of a commercial pharmaceutical product. The invention relates further to methods of preparing Form C and using it in the described pharmaceutical compositions.

Abstract: The present disclosure provides antimicrobial compounds, compositions comprising such antimicrobial compounds, and methods of their use, in particular, antibacterial compounds and antifungal compounds. In certain aspects, the antimicrobial compounds are effective against pathogens of hospital-acquired infections. In certain aspects, the antimicrobial compounds are effective against pathogens that are resistant to antibiotics. The antimicrobial compounds can be used in antibacterial compositions, antifungal compositions, antiseptic compositions and disinfectant compositions. The antimicrobial compounds can be used as adjuncts in antibacterial compositions and antifungal compositions.

Abstract: Process for the industrial synthesis of the compound of formula (I)

Abstract: This disclosure relates to novel detergents for use in various procedures including, for example, nucleic acid amplification reactions such as polymerase chain reaction (PCR). Methods for preparing the modified detergents are also described.

Abstract: The present invention relates to a novel method for producing an optically active ?-hydroxy-?-aminocarboxylic acid ester, the method comprising performing an asymmetric reduction reaction of a ?-keto-?-aminocarboxylic acid ester by use of a ruthenium complex as a catalyst.

Abstract: Nucleoside phosphinoamidite carboxylates and analogs are provided that have the structure of formula (III) wherein A is hydrogen, hydroxyl, lower alkoxy, lower alkoxy-substituted lower alkoxy, halogen, SH, NH2, azide or DL wherein D is O, S or NH and L is a heteroatom-protecting group, unsubstituted hydrocarbyl, substituted hydrocarbyl, heteroatom-containing hydrocarbyl, or substituted heteroatom-containing hydrocarbyl; B is a nucleobase; and one of R11 and R12 is a blocking group and the other is (IV) or (VI) in which W, X, Y, Z, R1 and n are as defined herein.

Abstract: A compound of formula (I): R?—O-A-O—R??, in which R? and R? are a hydrogen atom or a monovalent radical of formula (IIa), or a monovalent radical of formula (IIb), it being understood that at least one of the radicals R? or R? is not a hydrogen atom and that, when none of the radicals R? and R? is a hydrogen atom, R? and R? are identical, and in which A is a divalent radical of formula (III): —CH(X1)-[C(X2)(X3)]p-CH(X4) in which X1, X2, X3 and X4 are identical or different and are either a hydrogen atom or a methyl radical or an ethyl radical, and p is an integer greater than or equal to 1 and less than or equal to 6. Also the method for preparing the compound of formula (I) and to the use thereof in cosmetics and as a drug.

Abstract: A therapeutic and/or prophylactic agent for renal anemia comprising ALAs and an erythropoietin production promoter comprising ALAs.

Abstract: The present invention relates to a simple, economical and short synthesis for the class of compounds chemically belonging to amino acrylic acids of general formula I exhibiting both antibacterial and anti-plasmodium (anti-malarial) activity, in good yield and purity. Process for the preparation of said compound comprising heating amine (A) and pantolactone or substituted pantolactone (B) in a solvent selected from cyclohexane, benzene, toluene, xylene, diphenylether; anisole, dioxane, etc. at a temperature in the range of 110-150° C. for about 24 hrs followed by further raising the temperature of the mixture to a temperature in the range of 200-230° C. for period in the range of 15 to 25 min followed by cooling the crude reaction mixture to room temperature to obtain compound of general Formula I.

Abstract: A particulate material for the production of a cement foam which material includes particles including, attached to the particle surface, a surfactant which renders the particles hydrophilic, the surfactant including a moiety which is hydrolysable under alkaline conditions, which surfactant, after loss of the moiety by alkaline hydrolysis, renders the particles partially hydrophobic.

Abstract: In recognition of the need to develop novel therapeutic agents, the present invention provides novel histone deacetylase inhibitors. These compounds include an ester bond making them sensitive to deactivation by esterases. Therefore, these compounds are particularly useful in the treatment of skin disorders. When the compounds reaches the bloodstream, an esterase or an enzyme with esterase activity cleaves the compound into biologically inactive fragments or fragments with greatly reduced activity Ideally these degradation products exhibit a short serum and/or systemic half-life and are eliminated rapidly. These compounds and pharmaceutical compositions thereof are particularly useful in treating cutaneous T-cell lymphoma, neurofibromatosis, psoriasis, hair loss, skin pigmentation, and dermatitis, for example. The present invention also provides methods for preparing compounds of the invention and intermediates thereto.

Abstract: Provided are stable compositions comprising alkylating agents, including nitrogen mustards, that are suitable for topical use, and methods for treating skin disorders comprising topically administering the compositions.

Abstract: A compound which is the Michael addition reaction product of (A) a mono or polyacrylate of the formula R1(Ac)n wherein R1 is an organic radical having at least 2 carbon atoms, Ac is an acrylate radical of the formula CH2?CHC(O)O—, and n is from at least 1; with (B) is a primary or secondary amine of the formula R2NHR3, wherein R2 is a polyhydroxyl radical and R3 is H or an organic radical having at least one carbon atom is disclosed. The compound is useful as, for example, an oxygen barrier, flame retardant, polymer flocculant, surfactant, and/or high hydroxyl-functional intermediate.

Abstract: The present disclosure provides antimicrobial compounds, compositions comprising such antimicrobial compounds, and methods of their use, in particular, antibacterial compounds and antifungal compounds. In certain aspects, the antimicrobial compounds are effective against pathogens of hospital-acquired infections. In certain aspects, the antimicrobial compounds are effective against pathogens that are resistant to antibiotics. The antimicrobial compounds can be used in antibacterial compositions, antifungal compositions, antiseptic compositions and disinfectant compositions. The antimicrobial compounds can be used as adjuncts in antibacterial compositions and antifungal compositions.

Abstract: Esteramide compounds are useful solvents/coalescing agents for a variety of phytosanitary, cleaning, degreasing, stripping, lubricating, coating and pigment/ink compositions.

Abstract: Compounds which modulate quorum sensing in quorum sensing bacteria. Compounds of the invention inhibit quorum sensing and/or activate quorum sensing in various bacteria. Compounds that inhibit quorum sensing are particularly useful for inhibition of detrimental bacterial biofilm formation. Compounds that activate quorum sensing are particularly useful for promoting growth and biofilm formation of beneficial bacterial.

Abstract: Compounds and compositions comprising epoxyeicosatrienoic acid (EET) analogs that act as EET agonists and are useful as medications in the treatment of drug-induced nephrotoxicity, hypertension and other related conditions. Methods of making and using the compounds and compositions are further described.

Abstract: Amines and amine derivatives that improve the buffering range, and/or reduce the chelation and other negative interactions of the buffer and the system to be buffered. The reaction of amines or polyamines with various molecules to form polyamines with differing pKa's will extend the buffering range, derivatives that result in polyamines that have the same pKa yields a greater buffering capacity. Derivatives that result in zwitterionic buffers improve yield by allowing a greater range of stability.

Abstract: The present invention provides drug conjugates comprising 5-aminolevulinic acid (ALA), an aldehyde and a carboxylic acid that may function as a histone deacetylase inhibitor (HDACI). These conjugates may serve as co-drugs which release a plurality of active species in vivo. The novel drug conjugates may be used, for the treatment or prevention of cancer in PDT-dependent and/or PDT-independent (nonPDT) treatments, as well as for cosmetic uses. In addition the present invention provides novel uses for both the novel and known compounds. According to some embodiments, the present invention provides drug conjugates (co-drugs) comprising (i) ALA, (ii) an aldehyde and (iii) a carboxylic acid that may function as a histone deacetylase inhibitor (HDACO for the treatment of anemia and/or for the induction of erythropoiesis.

Abstract: A compound having the formula: X?N+(CH3)(CH2CH2OH)2[(CH2)n—COO—R1] and a polymer having the repeat unit: X?{—OCH2CH2—N+(CH3)[(CH2)n—CO—Y]—CH2CH2O—CO—NH—R2—NH—CO—}. R1 is an ester protecting group, R2 is an organic group, X is a halide, and n is a positive integer. Each Y is O?Z+ or O—R1, where Z+ is a cation from an aqueous base. A method of reacting N-methyldiethanolamine with an ?-halo-n-alkanoate ester to form the above compound.

Abstract: This invention relates to a novel crystalline polymorph of hexyl-5-aminolevulinate hydrochloride, referred to hereinafter as Form C, which is useful as precursor of a photo sensitizer in the photodynamic diagnosis and treatment of metabolically active cells related to diseases such as cancer of the uterus, cervix, vagina, rectum, colon, lower gastrointestinal tract; infection associated with cancer caused by human papilloma virus; non-cancerous lower gastrointestinal tract a human; inflammatory bowel disease; ulcerative colitis; Crohn's disease; inflammatory bowel syndrome; dysplasia of the female reproductive system; anus; penis; rosacea; and acne and which is suitable for use as the active ingredient of a commercial pharmaceutical product. The invention relates further to methods of preparing Form C and using it in the described pharmaceutical compositions.

Abstract: A a method for producing activated linear polymers and activatable branched polymers thereof, is carried out by a) reacting a linear nonpeptidic activatable polymer, chemically blocked at one end, with an azole ring activating group that provides a leaving group to produce an intermediate polymer of the general formula poly-lm; b) reacting said poly-lm with an alkylating agent to form an imidazolium salt of the general formula poly-1m+(alkyl)X-; and c) reacting said poly-lm +(alkyl)X with a linker molecule bearing at least two nucleophilic moieties to produce an activatable branched polymer derivative thereof. In some embodiments “poly” is a polymer selected from the group consisting of poly(alkylene oxides), poly(oxyethylated polyols), poly(olefinic alcohols), and polymers of alkylene oxide and propylene oxide; in some embodiments “Im +” is an imidazolium ion; and in some embodiments “X-” is an anionic counterion.

Abstract: The disclosure provides a series of 2-oxoamides based on dipeptides and pseudodipeptides, which were synthesized and their activities toward two human intracellular phospholipases A2 (GIVA CPLA 2 and GVIA 1PLA 2) and one human secretory phospholipase A2 (GV sPLA 2) were evaluated. Derivatives containing a free carboxyl group are selective GIVA cPLA 2 inhibitors. A derivative based on the ethyl ester of an ether pseudodipeptide is the first 2-oxoamide, which preferentially inhibits GVIA iPLA 2. The effect of 2-oxoamides on the generation of arachidonic acid from RAW 264.7 macrophages was also studied. It was found that selective GIVA cPLA 2 inhibitors preferentially inhibited cellular arachidonic acid release; in which one pseudodipeptide gave an IC50 value of 2 ?M.

Abstract: The invention relates to novel curcumin and tetrahydrocurcumin derivatives, which have been modified at one phenolic group to incorporate more-reactive groups. The curcumin and tetrahydrocurcumin derivatives are in the form of monomers, dimmers, and polymers.

Abstract: Compounds of the formula (I) in the form of a mixture of predominantly one diastereomer or in the form of pure diastereomers, Z1-Q-P*R0R1??(I), wherein: Z1 is a C-bonded, secondary phosphine group of the formula —P(R)2, wherein R is a hydrocarbon radical or O-atom(s)-containing heterohydrocarbon radical having 1 to 18 carbon atoms and optionally substituted by C1-C6-alkyl, trifluoromethyl, C1-C6-alkoxy, trifluoromethoxy, (C1-C4-alkyl)2-amino, (C6H5)3Si, (C1-C12-alkyl)3Si or halogen; Q is selected from the group consisting of: (i) an optionally substituted achiral aromatic group, wherein the achiral aromatic group is bonded directly to Z1 through a carbon atom of the achiral aromatic group and bonded directly to P*R0R1 through a carbon atom of the achiral aromatic group, and (ii) an optionally substituted C1-C4-alkylene group; P* is a chiral phosphorus atom; R0 is methyl; and R1 is a C-bonded optically enriched or optically pure chiral, mono- or polycyclic, nonaromatic hydrocarbon ring; and prepar

Abstract: The disclosure relates to medical devices coated with zein admixed with levulinic acid. The medical device may further include a therapeutic agent in contact with zein admixed with levulinic acid. Zein admixed with levulinic acid allows the therapeutic agent to be retained on the device during delivery and also controls the elution rate of the therapeutic agent following implantation. The disclosure further relates to methods of delivering a therapeutic agent on said medical devices as well as their use especially in the form of stents for prevention of restenosis.

Abstract: The invention provides formulations that contain an immunogenic or immunostimulatory cargo, delivery moiety and/or lipid, and a lipid that functions to reduce or prevent induction in a subject of an immune response which would otherwise occur when the immunogenic or immunostimulatory cargo, delivery moiety and/or lipid is administered to a subject as a component of an appropriate control formulation lacking the immune response reducing lipid. Specific immune response reducing lipids and uses thereof are further provided.

Abstract: Provided is a preventive and/or therapeutic agent for malaria, comprising, as an active ingredient, 5-acetamido-4-oxo-5-hexenoic acid (Alaremycin) or a derivative thereof. A preventive and/or therapeutic agent for malaria is used which comprises, as an active ingredient, Alaremycin or a derivative thereof represented by formula (I) (wherein R1 represents a hydroxy group, an amino group, or a substituted or unsubstituted straight chain or branched alkoxy group or alkylamino group having 1 to 8 carbons; R2 represents hydrogen, a substituted or unsubstituted straight chain or branched alkyl group having 1 to 8 carbons, or a substituted or unsubstituted aromatic group having 4 to 10 carbons; and R3 represents hydrogen or a methyl group).

Abstract: An industrially advantageous method for producing an optically active 1,2-bis(dialkylphosphino)benzene derivative of the present invention is provided. The method is characterized in that a phosphine-borane compound represented by the following general formula (1) is subjected to a deboronation reaction, followed by lithiation, then the reaction product is subjected to reaction with an alkyldihalogenophosphine represented by RaPX?2, and thereafter the reaction product is subjected to reaction with a Grignard reagent represented by RbMgX? to produce an optically active 1,2-bis(dialkylphosphino)benzene derivative (A). R1 and R2 respectively represent an alkyl group having 1 to 8 carbon atoms, and the number of carbon atoms is different between R1 and R2. Ra is either R1 or R2 and Rb is the other of R1 and R2. X, X?, and X? each represent a halogen atom.

Abstract: Described herein are compounds and compositions characterized, in certain embodiments, by conjugation of various groups, such as lipophilic groups, to an amino or amide group of an amino acid, a linear or cyclic peptide, a linear or cyclic polypeptide, or structural isomer thereof, to provide compounds of the present invention, collectively referred to herein as “APPLs”. Such APPLs are deemed useful for a variety of applications, such as, for example, improved nucleotide delivery. Exemplary APPLs include, but are not limited to, compounds of Formula (I), (II), (III), (IV), (V), and (VI), and salts thereof, as described herein: wherein m, n, p, R?, R1, R2, R3, R4, R5, R8, Z, W, Y, and Z are as defined herein.

Abstract: An amino acid-modified organopolysiloxane is provided. It has an amino acid derivative bonded to at least one silicon atom of the organopolysiloxane segment constituting the backbone of the organopolysiloxane via an amide bond represented by the following general formula (1): wherein X and Y are independently a C1-10 divalent hydrocarbon group; m is an integer of 0 to 4; Ra is hydrogen atom, a monovalent hydrocarbon group containing 1 to 4 carbon atoms, or an organic group represented by the following general formula (2): (wherein Rb is hydrogen atom, a C1-7 monovalent hydrocarbon group, an alkaline metal, or an alkaline earth metal, and Rc is independently hydrogen atom, hydroxy group, or a C1-10 monovalent hydrocarbon group optionally containing oxygen atom, sulfur atom, or nitrogen atom); and Z is an organic group represented by the general formula (2).

Abstract: Phospholipase A2 (PLA2) forms are expressed in spinal cord whose inhibition induces a potent antihyperalgesia. PLA2 inhibitor compounds are provided that include a common motif consisting of a 2-oxoamide with a hydrocarbon tail and a four carbon tether. The compounds block Group IVA calcium dependent PLA2 (cPLA2) and/or Group VIA calcium independent PLA2 (iPLA2) and/or Group V secreted PLA2 (sPLA2). Pharmaceutical compositions of compounds having cPLA2 inhibitory activity (but not iPLA2 or sPLA2 inhibitory activity) are useful in treating multiple sclerosis, while compositions of compounds having sPLA2 inhibitory activity (as well as iPLA2 and CPLA2 activity) are useful in treating spinal cord injuries (with related functional recovery).

Abstract: A compound which is the Michael addition reaction product of (A) a mono or polyacrylate of the formula R1(Ac)n wherein R1 is an organic radical having at least 2 carbon atoms, Ac is an acrylate radical of the formula CH2?CHC(O)O—, and n is from at least 1; with (B) is a primary or secondary amine of the formula R2NHR3, wherein R2 is a polyhydroxyl radical and R3 is H or an organic radical having at least one carbon atom is disclosed. The compound is useful as, for example, an oxygen barrier, flame retardant, polymer flocculant, surfactant, and/or high hydroxyl-functional intermediate.

Abstract: The invention relates to the cosmetic use, as a skin moisturizer, of a compound of formula (I): with (i) R1 and R2 represent a hydrogen atom or a C1-C6 alkyl group, or (ii) R1 and R2 can form, together with the nitrogen atom which bears them, a saturated heterocycle with 5 to 7 ring members; R5 representing a hydrogen atom or a (C1-C3) alkyl group; R6 representing a hydrogen atom or a (C1-C4) alkyl group; R3 represents a hydrogen atom or a (C1-C6) alkyl group, or —OR3 represents a phosphate group; it being possible for the two groups R3 to form, together, an isopropylidene group; R4 represents a hydrogen atom or —OR4 represents a phosphate group; and the salts, solvates and isomers thereof. The invention also relates to a cosmetic composition comprising a compound (I) and the corresponding new compounds.

Abstract: There is disclosed use of hyperbranched polyester amides as a foamer to stabilize mixtures of oil and water especially for mixtures found in gas and/or oil wells to facilitate extraction of the well contents.

Abstract: A halogenating agent is added to a mixture including a base, a fluoroalkylcarboxylic acid derivative and an acrylate derivative to produce a fluoroaclyacetic acid derivative represented by the following Formula (3): wherein Rf represents a fluorine containing alkyl group, R1 and R2 represent a hydrogen atom, an alkyl group, a cycloalkyl group, an aryl group, an arylalkyl group or an acyl group, or together represent an atomic group that forms a 5- or 6-membered ring containing a nitrogen atom to which R1 and R2 are bonded; R3 represents a hydrogen atom, an alkyl group, a cycloalkyl group, an aryl group, or an arylalkyl group; and R4 represents an alkyl group, a cycloalkyl group, an aryl group, or an aryl alkyl group.

Abstract: This disclosure relates to novel detergents for use in various procedures including, for example, nucleic acid amplification reactions such as polymerase chain reaction (PCR). Methods for preparing the modified detergents are also described.

Abstract: Amines and amine derivatives that improve the buffering range, and/or reduce the chelation and other negative interactions of the buffer and the system to be buffered. The reaction of amines or polyamines with various molecules to form polyamines with differing pKa's will extend the buffering range, derivatives that result in polyamines that have the same pKa yields a greater buffering capacity. Derivatives that result in zwitterionic buffers improve yield by allowing a greater range of stability.

Abstract: Amines and amine derivatives that improve the buffering range, and/or reduce the chelation and other negative interactions of the buffer and the system to be buffered. The reaction of amines or polyamines with various molecules to form polyamines with differing pKa's will extend the buffering range, derivatives that result in polyamines that have the same pKa yields a greater buffering capacity. Derivatives that result in zwitterionic buffers improve yield by allowing a greater range of stability.

Abstract: The present invention relates to a process for preparing 2-fluoroacyl-3-aminoacrylic acid derivatives by reacting fluorinated carboxylic acids with dialkylaminoacrylic acid derivatives and acid halides.

Abstract: The invention relates to amino and hydroxy-functional polyesters, wherein the amine is in the form of aspartic acid esters functionality, and wherein the amino and hydroxy-functional polyester has (a) a molecular weight (Mn) of at least about 500, (b) an acid value of about 5 or less, (c) a hydroxyl value of about 30 or more, and (d) an amine value of about 30 or more, and (e) an amine functionality of less than 1.8. Preferably, the compound includes molecules having on the average: at least 1 secondary amino group as an aspartate, and/or at least 1 hydroxy group, and an average total functionality of about 1.8 or higher. More preferably, the molecular weight of the amino and hydroxy-functional polyesters is between 204 and 10,000 and preferably between 482 and 5000.

Abstract: The invention relates to amino and hydroxy-functional compounds other than polyesters, wherein the compound includes an amine in the form of aspartic acid esters functionality, and wherein the amino and hydroxy-functional compound has (a) a molecular weight (Mn) of at least about 500, (b) an acid value of about 5 or less, (c) a hydroxyl value of about 30 or more, and (d) an amine value of about 30 or more. Preferably, the compound includes molecules having on the average: at least 1 secondary amino group as an aspartate, and/or at least 1 hydroxy group, and an average total functionality of about 1.8 or higher.

Abstract: The present invention relates to a process for preparing hydrochloride-free 2-dihaloacyl-3-aminoacrylic esters by reacting acid fluorides with dialkylaminoacrylic acid derivatives.