Abstract: A method for preparing a compound of Formula 1 comprising contacting a compound of Formulae 2 and 3 in the presence of a palladium source, a ligand, a base and carbon monoxide wherein R1, R2, X and R3 are as defined in the disclosure. A method for preparing a compound of Formula 5 wherein R1, R2, R3, R4, R5, R6 and Z are as defined in the disclosure, using a compound of Formula 1 characterized by preparing a compound of Formula 1 by the method disclosed above or using a compound of Formula 1 prepared by the method above.

Abstract: A solvent-free mechanical process of reacting amine compounds with acetylating agents resulting in amides such as acetaminophen is described.

Abstract: The present disclosure generally relates to a new process for the preparation of high purity 5-nitro-isophthalamide compounds, which are useful as intermediates for the preparation of imaging agents, such as iodinated x-ray contrast imaging agents like ioversol, iohexyl and iopamidol.

Abstract: The invention relates to new ?-hydroxyalkylamides, to a method for production of same and to the use of same.

Abstract: Novel processes for the preparation of a compound of Formula I-2 substantially free of the 5,6-trans isomer: wherein R2, R3 and R4 are as defined in the specification are provided. Novel intermediates for the preparations of isomer free Prostaglandins and derivatives thereof are also provided.

Abstract: Provided are a benzamide derivative as shown in formula (I) or a pharmaceutically acceptable salt thereof, and the preparation method and use thereof for preparing a medicine for treating cancer, wherein the group definitions of formula (I) are as set out in the description.

Abstract: The present patent application relates to an alternative process for the preparation of amino derivatives. In particular, the present application relates to an improved process for the manufacture of Lacosamide (LCM), (R)-2-acetamido-N-benzyl-3-methoxypropion-amide, which is useful as an anticonvulsive drug. In a particular aspect, the present invention relates to a process of manufacture of optically enriched (R)-2-acetamido-N-benzyl-3-methoxypropion-amide (I) comprising resolution of 2-acetamido-N-benzyl-3-methoxypropion-amide (II).

Abstract: A method for preparing a compound of Formula 1 comprising contacting a compound of Formulae 2 and 3 in the presence of a palladium source, a ligand, a base and carbon monoxide wherein R1, R2, X and R3 are as defined in the disclosure. A method for preparing a compound of Formula 5 wherein R1, R2, R3, R4, R5, R6 and Z are as defined in the disclosure, using a compound of Formula 1 characterized by preparing a compound of Formula 1 by the method disclosed above or using a compound of Formula 1 prepared by the method above.

Abstract: The present invention relates to a quinic acid derivative, preparation process of the same and pharmaceutical uses thereof. The quinic acid derivative has a quinic acid-like structure which binds to CD28, blocks T-cell signal 2 pathway via CD28, and suppresses T-cell activation. The C-1 carboxyl group, the C-3 hydroxyl group and the C-4 hydroxyl group of quinic acid are modified to attenuate the cytotoxicity of the quinic acid derivative. The preparation process of the quinic acid derivative comprises 2 steps of: treating quinic acid with the first reagent in the presence of the acid catalyst to form an immediate; and treating the immediate with the second reagent to from the quinic acid derivative. With the ability to suppress T-cell activation, the quinic acid derivative is used to treats an autoimmune disease, an allergy, transplant rejection or other related immune disorder.

Abstract: The invention relates to novel ?-hydroxyalkylamides, to a method for their production and to the use thereof.

Abstract: Disclosed is a method involving reacting a deprotonated mono- or dialkanol amine with one or more C4 to about C75 fatty acid monoalcohol esters.

Abstract: A carboxamide can be produced in a high yield by a method for producing a carboxamide, for example, represented by formula (4): (wherein R1 and R3 are as defined below), the method comprising a step of allowing a carboxylic acid ester represented by formula (1): (wherein R1 represents an optionally substituented C1-C20 hydrocarbon group or an optionally substituented C3-C20 heterocyclic group, and R2 represents an optionally substituented C1-C20 hydrocarbon group), an amine represented by formula (2): R3—NH2??(2) (wherein R3 represents a hydrogen atom or an optionally substituented C1-C20 hydrocarbon group), and a formamide compound represented by formula (3): (wherein R3 is as defined above) to react in the presence of a metal alkoxide.

Abstract: The present invention is directed to compounds, intermediates and methods for making valerenic acid and its derivatives as well as the use of such compounds as GABAA receptor ligands.

Abstract: It is described a process for the opening of lactone or lactam rings useful in the synthesis of pharmaceutically active compounds and the intermediates thereof, particularly Aliskiren. It has found that by selecting a type of solvent it is possible to obtain excellent yields and high optical and chemical purity of the isolated products.

Abstract: The present disclosure generally relates to a new process for the preparation of high purity 5-nitro-isophthalamide compounds, which are useful as intermediates for the preparation of imaging agents, such as iodinated x-ray contrast imaging agents like ioversol, iohexyl and iopamidol.

Abstract: The invention relates to a process for the preparation of formamides by reacting aromatic amines with a formic acid ester in the presence of a catalyst, wherein the catalyst is a phosphorus-containing acid or a Lewis-acidic metal salt.

Abstract: The invention relates to a process for continuously preparing N-alkyl(meth)acrylamides by reacting alkyl(meth)acrylates with high-boiling amines. A catalyst activation and specific workup technique achieve product qualities which have not been achieved to date. In addition, very high space-time yields and overall yields can be achieved.

Abstract: The present invention relates to a process for preparing substituted 2-aminobiphenyls and to a process for preparing (Het)arylamides of such 2-aminobiphenyls.

Abstract: A process for producing high purity 3-hydroxypropionic acid from a fermentation cell broth is described. The 3-hydroxypropionic acid can be converted to a variety of products, such as acrylamide, 3-hydroxypropionic esters, acrylic esters, and 3-HP amide. This process features a high degree of product flexibility, limited or no solvent recycle, discrete waste streams, an efficient water removal process, and efficient recovery of products and solvents with proven and scalable equipment.

Abstract: The invention provides compound of the general formula: in which each X independently represents a polymer chain; n represents an integer greater than 1; Q represents a linker; Y represents an amide group; and Z represents either —CH.(CH2L)2 or —C(CH2L)(?CH2), in which each L independently represents a leaving group. The compounds are useful reagents for the conjugation of polymers to proteins, the resulting conjugates being novel and also forming part of the invention.

Abstract: The preparation of cyclohexadienes from one or more plant oils is disclosed. The cyclohexadiene can be used to form polymers or derivatized to form other monomers that can be used to form polymeric materials.

Abstract: A process for the preparation of 4-iodo-3-nitrobenzamide free from the impurities formed due to nucleophilic substitution of the labile iodo group is disclosed.

Abstract: Provided are a benzamide derivative as shown in formula (I) or a pharmaceutically acceptable salt thereof, and the preparation method and use thereof for preparing a medicine for treating cancer, wherein the group definitions of formula (I) are as set out in the description.

Abstract: A process for the preparation of 4-iodo-3-nitrobenzamide free from the impurities formed due to nucleophilic substitution of the labile iodo group is disclosed.

Abstract: The invention relates to novel guanidine derivatives in the cinnamic series of general formula (I): The invention also relates to the process for preparing said guanidine derivatives and also to synthetic intermediates. Finally, the invention relates to the use of the guanidine derivatives for the preparation of compositions with anti-glycation properties, especially in cosmetology.

Abstract: A process for manufacturing dialkyl lactamide including reacting lactide and dialkylamine selected from one or more of dimethylamine, diethylamine, and methylethylamine to form a reaction mixture which includes dialkyl lactamide selected from N,N-dimethyl lactamide, N,N-diethyl lactamide, and N,N-methylethyl lactamide, N,N-dialkyl lactoyl lactamide, and dialkylamine, subjecting the reaction mixture to a separation step to form a product stream including N,N-dialkyl lactamide, a first recycle stream including dialkylamine and a second recycle stream including N,N-dialkyl lactoyl lactamide, feeding the recycle streams to the reaction step, and isolating the product stream. The process allows the manufacture of N,N-dimethyl lactamide, N,N-diethyl lactamide, and N,N-methylethyl lactamide on a commercial scale.

Abstract: To provide a water/oil repellent agent and a water/oil repellent composition which are capable of imparting sufficient water/oil repellency to the surface of an article and which have low environmental impact. One comprising a reaction product obtained by reacting a fluorinated alcohol or amine having a polyfluoroalkyl moiety having at most 6 carbon atoms with a polyisocyanate compound, which is, when applied to an article, capable of imparting sufficient water/oil repellency, while presenting little environmental impact. When applied to an article, the water/oil repellent composition of the present invention is capable of imparting a high quality water/oil repellency to the article.

Abstract: Provided are films made from copolyesters having improved oil repellency as compared to conventional copolyesters. The copolyesters are derived from certain perfluorinated monomers.

Abstract: Disclosed are fluorovinyl ether functionalized aromatic diesters and derivatives thereof. The compounds disclosed have utility as functionalized monomers and comonomers in polyesters, polyamides, and the like. It has been found that incorporation of the monomers into polymers provides improved soil resistance to shaped articles produced from the polymers.

Abstract: A process for preparing N,N-dimethylacetamide (DMAC) by continuously reacting methyl acetate (MeOAc) with dimethylamine (DMA) in the presence of a basic catalyst, wherein MeOAc is used in the form of a methanolic solution which is obtained as a by-product in the preparation of polyTHF by transesterifying polyTHF diacetate with methanol.

Abstract: A mutant hydrolase optionally fused to a protein of interest is provided. The mutant hydrolase is capable of forming a bond with a substrate for the corresponding nonmutant (wild-type) hydrolase which is more stable than the bond formed between the wild-type hydrolase and the substrate. Substrates for hydrolases comprising one or more functional groups are also provided, as well as methods of using the mutant hydrolase and the substrates of the invention. Also provided is a fusion protein capable of forming a stable bond with a substrate and cells which express the fusion protein.

Abstract: This invention provides the compound having the structure wherein n is 1-10; X is C—R11 or N; wherein R11 is H, OH, SH, F, Cl, SO2R7, NO2, trifluoromethyl, methoxy, or CO—R7, wherein R7 is alkyl, alkenyl, alkynyl, C3-C8 cycloalkyl, or aryl; Z is R2 is H or NR3R4, wherein R3 and R4 are each independently H, C1-C6 alkyl, or C3-C8 cycloalkyl; R5 is OH or SH; and R6, R12, R13, and R14 are each independently H, OH, SH, F, Cl, SO2R15, NO2, trifluoromethyl, methoxy, or CO—R15, wherein R15 is alkyl, alkenyl, alkynyl, C3-C8 cycloalkyl, or aryl, or a salt of the compound, which is useful in the treatment of tumors.

Abstract: The presently disclosed subject matter provides a method of synthesizing prostaglandins and prostaglandin analogs comprising the ring closing metathesis of compounds of Formula (I). Also provided are novel compounds of Formula (I) and Formula (II). In addition to their use as synthetic intermediates in the presently disclosed methods, compounds of Formula (II) can be used as prostaglandin and/or prostaglandin analog prodrugs.

Abstract: The invention provides methods and compositions for preparing lisdexamfetamine and salts thereof. More particularly, the invention provides, for example, methods of preparing lisdexamfetamine from D-amphetamine.

Abstract: A process for preparing N,N-dimethylacetamide (DMAC) by continuously reacting methyl acetate (MeOAc) with dimethylamine (DMA) in the presence of a basic catalyst, wherein MeOAc is used in the form of a methanolic solution and the continuous distillative workup is effected in such a way that methanol and any other low boilers are initially removed overhead in a column A and the bottom effluent of column A is fed to a column B in which DMAC is removed via a side draw a purity of ?99.7% by weight.

Abstract: The invention relates to a continuous method for producing amides of aromatic carboxylic acids by reacting at least one carbonic acid ester of formula (I) R3—OOOR4, wherein R3 represents an optionally substituted aromatic hydrocarbon group with 5 to 100 carbon atoms and R4 represents a hydrocarbon group with 1 to 30 carbon atoms, with at least one amine of formula (II) HNR1R2, wherein R1 and R2 independently represent hydrogen or a hydrocarbon group with 1 to 100 C atoms, in a reaction tube the longitudinal axis of which extends in the direction of propagation of the microwaves of a monomode microwave applicator, under microwave irradiation to form carboxamide.

Abstract: Cobalt(II) complexes of the D2-symmetric chiral porphyrins are effective catalysts for asymmetric cyclopropanation reactions with succinimidyl diazoacetate. The Co-catalyzed reaction is suitable for various olefins, providing the corresponding cyclopropane succinimidyl esters in high yields and excellent diastereo- and enantio-selectivity.

Abstract: The invention relates to a process for continuously preparing N-alkyl(meth)acrylamides by reacting alkyl (meth)acrylates with high-boiling amines. A catalyst activation and specific workup technique achieve product qualities which have not been achieved to date. In addition, very high space-time yields and overall yields can be achieved.

Abstract: The present invention relates to a method for synthesizing a pharmaceutically acceptable acid addition salt of (1S, 2R)-milnacipran comprising the following successive steps: (a) reaction of phenylacetonitrile and of (R)-epichlorhydrin in the presence of a base containing an alkaline metal, followed by a basic treatment, and then by an acid treatment in order to obtain a lactone; (b) reaction of said lactone with MNEt2, wherein M represents an alkaline metal, or with NHEt2 in the presence of a Lewis acid-amine complex, in order to obtain an amide-alcohol; (c) reaction of said amide-alcohol with thionyl chloride in order to obtain a chlorinated amide; (d) reaction of said chlorinated amide with a phthalimide salt in order to obtain a phthalimide derivative; (e) hydrolysis of the phthalimide group of said phthalimide derivative in order to obtain (1S, 2R)-milnacipran, and (f) salification of (1S, 2R)-milnacipran in a suitable solvent system in the presence of a pharmaceutically acceptable acid.

Abstract: The present invention provides a method for the synthesis of radioiodinated compounds which is advantageous over prior art methods. Using a hydrazine or an aminoxy in place of a primary amine for indirect radioiodination facilitates a much quicker reaction thus reducing reaction time and increasing the yield. In addition, where there are primary amines in the molecule to be radioiodinated, such as the N-terminus of a peptide or lysine residues, reaction at the hydrazine or aminoxy is greatly favoured.

Abstract: The present invention includes methods/processes and intermediates for preparing compounds having structural Formula (I): wherein X is alkyl, substituted alkyl, alkenyl, substituted alkenyl, heteroalkyl, substituted heteroalkyl, heteroalkenyl, or substituted heteroalkenyl.

Abstract: A compound of general formula (I). A process for preparing this compound. A fungicidal composition comprising a compound of general formula (I). A method for treating plants by applying a compound of general formula (I) or a composition comprising it.

Abstract: The invention relates to new ?-hydroxyalkylamides, to a method for production of same and to the use of same.

Abstract: Disclosed are fluorovinyl ether functionalized aromatic diesters and derivatives thereof. The compounds disclosed have utility as functionalized monomers and comonomers in polyesters, polyamides, and the like. It has been found that incorporation of the monomers into polymers provides improved soil resistance to shaped articles produced from the polymers.

Abstract: Provided herein are novel bridged cyclic derivatives of the general formula (I), their analogs, tautomeric forms, stereoisomers, polymorphs, solvates, intermediates, pharmaceutically acceptable salts, pharmaceutical compositions, metabolites and prodrugs thereof. These compounds can inhibit HDACs and are useful as therapeutic or ameliorating agent for diseases that are involved in cellular growth such as malignant tumors, autoimmune diseases, skin diseases, infections, inflammation, neurode-generative disorders etc.

Abstract: A process for manufacturing dialkyl lactamide including reacting lactide and dialkylamine selected from one or more of dimethylamine, diethylamine, and methylethylamine to form a reaction mixture which includes dialkyl lactamide selected from N,N-dimethyl lactamide, N,N-diethyl lactamide, and N,N-methylethyl lactamide, N,N-dialkyl lactoyl lactamide, and dialkylamine, subjecting the reaction mixture to a separation step to form a product stream including N,N-dialkyl lactamide, a first recycle stream including dialkylamine and a second recycle stream including N,N-dialkyl lactoyl lactamide, feeding the recycle streams to the reaction step, and isolating the product stream. The process allows the manufacture of N,N-dimethyl lactamide, N,N-diethyl lactamide, and N,N-methylethyl lactamide on a commercial scale.

Abstract: The present invention relates to a novel manufacturing process and novel intermediates useful in the synthesis of pharmaceutically active compounds, especially rennin inhibitors such as Aliskiren. The invention describes a preparation of enantiomerically pure 8-aryloctanoic acids of general formula I from readily available key intermediate, chiral cis-diacid of formula II, aziridine of formula XI and a monocyclic compound of formula III.

Abstract: The present invention relates to compounds useful as pharmaceutical intermediates, to processes for preparing the intermediates, to intermediates used in the processes, and to the use of the intermediates in the preparation of pharmaceuticals. In particular, the present invention concerns enantiomerically pure trans-cyclopropane carboxylic acid derivatives, processes for preparing the carboxylic acid derivatives and their use in preparing pharmaceuticals.

Abstract: A process for reacting, in the presence of a particular calcium containing catalyst, an amine having an active hydrogen and one or more of a fatty acid ester or a fatty acid.

Abstract: The present invention is directed to certain hydroxamate derivatives that are useful in the treatment of hepatitis C. These compounds are also inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase activity. Pharmaceutical compositions and processes for preparing these compounds are also disclosed.