Abstract: Non-natural amino acids such as 2-alkylated amino acids allow for the synthesis of a wider variety of peptidal and non-peptidal pharmaceutically active agents. In one embodiment, the present invention provides methods of preparing 2-alkylcysteine derivatives. In another embodiment, the method comprises forming a 2-alkylcysteine derivative from a cysteine derivative in the presence of a phase transfer catalyst. In particular, the present invention provides methods for preparing 2-methylcysteine derivatives. The present invention also discloses a method of preparing a class of iron chelating agents related to desferrithiocin, all of which contain a thiazoline ring. In one aspect, an aryl nitrile or imidate is condensed with cysteine or a 2-alkyl cysteine. The present invention also relates to the preparation of 4,5-dihydro-2-(2,4-dihydroxyphenyl)-4-alkyl-thiazole-4-carboxylic acids, such as 4,5-dihydro-2-(2,4-dihydroxyphenyl)-4-methyl-thiazole-4-carboxylic acid.

Abstract: This invention relates to attachment chemistries for binding macromolecules to a substrate surface or to other conjugation targets. More particularly, this invention relates to attachment chemistries involving branched or linear structures having one or more hydrazide attachment moieties for binding the macromolecules to a substrate surface, or for other conjugation reactions. Novel modifying reagents are provided for the introduction of protected hydrazide attachment moieties or precursor forms of such hydrazides to the macromolecule, either as a single hydrazide or as multiple hydrazides.

Abstract: Disclosed are blue, diol anthraquinone blue colorant compounds having excellent thermal stability and which can be reacted into or copolymerized with polyester thus providing a blue-colored polyesters useful for manufacturing a variety of shaped articles such as photographic film base, particularly roentgenographic (X-ray) film. Also disclosed are blue anthraquinone colorant compounds which contain two ethylenically-unsaturated (vinyl), photopolymerizable radicals which may be derived from the aforesaid diol anthraquinone compounds. The anthraquinone colorant compounds containing two ethylenically-unsaturated may be reacted into or copolymerized (or cured) with ethylenically-unsaturated monomers to produce colored vinyl polymers.

Abstract: Charge transport compounds are described that have a multiple number of hydrazone-bridged heterocyclic groups (especially julolidine groups, carbazole groups, triarylamine groups and (N,N-disubstituted)arylamine groups such as dialkarylamine groups (e.g. dimethylphenylamine; methylethylphenylamine, dipropylphenylamine, ethylepropylphenylamine, ethylbutylnaphthylamine, etc.), alkyldiarylamine groups (e.g. methyldiphenylamino, ethyldiphenylamino, etc), and triarylamino groups (e.g., triphenyl amino, trinaphthylamino, etc)) connected by a central bridging group.

Abstract: Charge transport compounds are described that have a multiple number of hydrazone-bridged heterocyclic groups (especially julolidine, carbazole and/or triarylmethane groups) connected by a central bridging group.

Abstract: The present invention relates to benzoxazinones of formula I: or stereoisomeric forms or mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HIV reverse transcriptase, and to pharmaceutical compositions and diagnostic kits comprising the same, methods of using the same for treating viral infection or as an assay standard or reagent, and intermediates and processes for making the same.

Abstract: Novel triphenylmethane dyes or colorants with sterically hindered fugitive amine counter ions are provided as durable, storage-stable, and excellent coloring and shading printing inks. Ink compositions are disclosed which provide improvements in long-term storage capabilities, particularly within alkaline environments, extremely effective colorations of cellulose-based substrates, and lower cost over those of the prior art. The preferred dyes or colorants are triphenylmethane polymeric colorants which are capped with cyclic anhydride and the preferred sterically hindered amine counter ions are those based on low molecular weight fugitive tertiary amines, such as N,N-dimethylethanolamine. Compositions comprising water soluble or emulsion resins as diluents for lowered viscosity and lower overall cost are also contemplated. Furthermore, compositions comprising the inventive colorant and other pigments, dyes, surfactants, preservatives, and other colorants are contemplated.

Abstract: Amino acids are derivatized for use in peptide synthesis by conversion to N-carboxyanhydrides that are N-protected by either a trityl or a phenylfluorenyl group.

Abstract: A method of producing an ether-type thio-phospholipid of the formula (I): ##STR1## wherein: n is an integer of 13 to 17;A is C.sub.14 -C.sub.20 acyl group;G is a group selected from the group consisting of: ##STR2## which is useful as synthetic substrate of cytosolic phospholipase A.sub.2 inhibitors, said method being applicable to mass production of the compound (I), intermediates therefor and the preparation of the same are provided.

Abstract: New trityl linkers for use in solid phase synthesis comprise compounds of formula II ##STR1## wherein R.sub.4 is alkyl (e.g. C.sub.1-4 alkyl), halogen, NO.sub.2, or hydrogen;Z is a coupling group chosen from acylamido, acyloxy, amino, halogen, thiol or hydroxyl,where acyl is the residue of a carboxylic acid or a residue of formula R.sub.5 CO where R.sub.5 is an organic group;Y is H, a reactive functional group or an attachment to a solid phase;W is O when Y is H or a reactive functional group, or W is --NH--, or --NR.sub.6 --(urethane) when Y is an attachment to a solid phase,where R.sub.6 is an organic group and,each R which, may be the same or different, is C(O)NR.sub.7 R.sub.8, CF.sub.3, F or Cl wherein each R.sub.7 and R.sub.8, which may be the same or different, is H or C.sub.

Abstract: The present invention pertains to a process for the preparation of Compound (4) through the below-described reaction route: ##STR1## wherein R.sup.1 and R.sup.2 each represents H, halogen, OH or C.sub.1-6 alkyl group; X and Y each represents a protected amino group and n stands for 0 to 4. According to the above process, an aminotetralone derivative which is an intermediate useful for an industrial preparation of a camptothecin derivative can be obtained in a convenient manner and in a high yield.

Abstract: The present invention is directed to the process of preparing a peptide comprising reacting a first amino acid or peptide with an amino acid fluoride of the formula: ##STR1## or the acid fluoride salts thereof wherein BLK is an N-amino protecting groupAA is an amino acid residue andX is H or a protecting group useful,and the first amino and peptide have a free amino group and a blocked carboxy end.

Abstract: The present invention related to novel (R)-dimethyl N-tritylaspartate and novel (R)-alkyl N-trityl-4-oxo-5-phosphononorvalinate derivatives which are useful in the preparation of the class of beta-ketophosphonate NMDA antagonists.

Abstract: Compounds of formula I are described, ##STR1## wherein n is equal to one or two, R.sub.1 stands for hydrogen or an amino protecting group, R.sub.2 represents hydrogen or a carboxyl protecting group and R.sub.3 4-methyltriphenylmethyl, 4,4'-dimethyltriphenylmethyl, 4,4',4"-trimethyltriphenylmethyl. Furthermore described are compounds of formula I which are reactive and suitable for coupling reactions and are derived from I with R.sub.2 =H by activation of the carboxyl group.The compounds mentioned above can be used as starting materials for the synthesis of peptides. They are more suitable than analogous compounds of formula I, wherein R.sub.3 represents hydrogen or a carbamoyl protecting group used hitherto.

Abstract: Ether variant lipids bound to phosphoramidites are disclosed. These can be used to create oligonucleotides that are linked to stable lipid-like units. For example, dialkyl glycerols are linked to phosphoramidites.

Abstract: A compound of the formula ##STR1## or the acid fluoride salts thereof wherein BLK is an N-amino protecting group or hydrogenAA is an amino acid residue andX is H or a protecting group useful as a coupling agent in peptide synthesis.

Abstract: Compounds of the formula I, ##STR1## in which 'R.sub.1 is an amino protective group, and n stands for 1 or 2, R.sub.1 denotes hydrogen or an amino protective group, R.sub.2 denotes hydrogen or a carboxyl protective group and R.sub.3 denotes triphenylmethyl, 4-monomethoxy-trityl or 4,4'-dimethoxy-trityl, and reactive carboxylic acid derivatives of such compounds of the formula I in which R.sub.2 stands for hydrogen, are described.These compounds can be used as starting materials for the preparation of peptides. They are more suitable for this than are analogous compounds of the formula I in which R.sub.3 denotes hydrogen or one of the carbamoyl protective groups hitherto customary.

Abstract: Color formers of the general formula ##STR1## in which --independently of one another-- R.sup.1 and R.sup.2 are hydrogen, halogen, alkyl, aralkyl etc.,Y.sup.1 and Y.sup.2 are alkyl, aryl, cycloalkyl or aralkyl,X.sup.1 is alkyl, alkenyl, cycloalkyl, aralkyl etc.,X.sup.2 is H, alkyl, alkenyl, cycloalkyl etc.X.sup.1 with X.sup.2 with the inclusion of the nitrogen atom carrying them can form a saturated or unsaturated 5- or 6-membered heterocyclic ring, andfurther isocyclic or heterocyclic rings can be fused with the rings A, B and C, upon incorporation in recording materials based on acid developers, show a particularly advantageous migration behaviour. Deep blue, green-blue, green, violet or red shades which have excellent sublimation and light fastness are obtained.

Abstract: Compounds of the general formula ##STR1## in which the symbols have the meaning given in the description, are highly suitable as color formers in recording materials based on acid developers. They give deep blue, green-blue, green, violet or red shades which have excellent sublimation and light fastness.

Abstract: An improvement is described in the synthesis method for N.sup..alpha. -trityl-N.sup.G -trityl arginine within a process for preparing N.sup..alpha. -fluorenylmethoxycarbonyl-N.sup.G -trityl-arginine from arginine, comprising:a) forming N.sup..alpha. -trityl-N.sup.G -trityl-arginineb) selectively detaching the trityl group from the .alpha.-NH.sub.2 andc) introducing the fluorenylmethoxycarbonyl group in its place.The improvement consists of preparing the N.sup..alpha. -trityl-N.sup.G -trityl-arginine by solubilizing the arginine in an aprotic organic solvent by tri-alkylsilylation both of the amino nitrogen and of the carboxyl group, followed by tritylation, with trityl chloride, of the .alpha.-amino nitrogen, and of the guanidino group after deprotonating this latter with a bicyclic guanidine. The new improved process can also lead to variable quantities of the arginine analogue di-tritylated at the guanidino group, namely N.sup..alpha. -fluorenylmethoxycarbonyl-N.sup.G -di-trityl-arginine.

Abstract: A method is described for substituting at least one hydrogen atom originally present in the guanidino group of a compound of general formula (I) ##STR1## where R is any substituted or unsubstituted residue, by a group R.sub.1 where R.sub.1 is an unsubstituted or substituted, linear or branched alkyl, consisting of:a) silylating the guanidino group and any other silylatable functional groups present within the R group andb) alkylating the product obtained in step a) with a mixture consisting of the alkyl halide R.sub.1 -X and an organic base containing a tertiary nitrogen.

Abstract: A novel N-substituted peptidyl compound represented by the general formula (1): ##STR1## where R.sub.1 is a straight-chained or branched acyl group having 2-10 carbon atoms, a branched, cyclic or partly branched cyclic alkyloxycarbonyl group having 4-15 carbon atoms, a substituted or unsubstituted benzyloxycarbonyl group, a 2,2,2-trichloroethyloxycarbonyl group, a 2-(trimethylsilyl)ethyloxycarbonyl group, a p-toluensulfonyl group, an o-nitrophenylsulfenyl group, a diphenylphosphonothioyl group, a triphenylmethyl group, a 2-benzoyl-1-methylvinyl group or a 4-phenylbutyryl group; R.sub.2 is a hydrogen atom or when taken together with R.sub.1, may form a phthaloyl group; R.sub.3 is an isobutyl group, a n-butyl group or an isopropyl group; R.sub.4 is a butyl group, a benzyl group or a methylthioethyl group; and R.sub.5 is a hydrogen atom or a chloromethyl group, which inhibits the activity of cysteine proteinases.

Abstract: An improvement is described in the synthesis method for N.sup..alpha. -trityl-N.sup.G -trityl arginine within a process for preparing N.sup..alpha. -fluorenyl-methoxycarbonyl-N.sup.G -trityl-arginine from arginine, comprising:a) forming N.sup..alpha. -trityl-N.sup.G -trityl-arginineb) selectively detaching the trityl group from the .alpha.-NH.sub.2 andc) introducing the fluorenylmethoxycarbonyl group in its place.The improvement consists of preparing the N.sup..alpha. -trityl-N.sup.G -trityl-arginine by solubilizing the arginine in an aprotic organic solvent by tri-alkylsilylation both of the amino nitrogen and of the carboxyl group, followed by tritylation, with trityl chloride, of the .alpha.-amino nitrogen, and of the guanidino group after deprotonating this latter with a bicyclic guanidine. The new improved process can also lead to variable quantities of the arginine analogue di-tritylated at the guanidino group, namely N.sup..alpha. -fluorenylmethoxycarbonyl-N.sup.G -di-trityl-arginine.

Abstract: A reactive dye of the formulaD--U--R).sub.nin which D is the radical of an anthraquinone, phthalocyanine, formazane, azomethine, dioxazine, phenazine, stilbene, triphenylmethane, xanthene, thioxanthone, nitroaryl, naphthoquinone, pyrenequinone or perylenetetracarbimide dye; U is --CO-- or --SO.sub.2 --; R is a radical of the formula ##STR1## Z is sulfatoethyl, .beta.-thiosulfatoethyl, .beta.-phosphatoethyl, .beta.-acetoxyethyl, .beta.-halogenoethyl or vinyl; alk is a polymethylene radical having 1 to 6 C atoms or its branched isomers; Y is hydrogen, chlorine, bromine, fluorine, hydroxyl, sulfato, C.sub.1 -C.sub.4 -alkanoyloxy, cyano, carboxyl, alkoxycarbonyl having 1 to 5 C atoms, carbamoyl or a radical --SO.sub.2 --Z in which Z is as defined above; V is hydrogen or C.sub.1 -C.sub.4 -alkyl which is unsubstituted or substituted by carboxyl, sulfo, C.sub.1 -C.sub.2 -alkoxy, halogen or hydroxyl;or a radical ##STR2## in which Z, alk and Y are as defined above; R.sub.1 is hydrogen or C.sub.1 -C.sub.

Abstract: Oligonucleotide functionalizing reagents are disclosed which are useful in introducing sulfhydryl, amino and additional hydroxyl groups into oligonucleotides. The reagents are substantially linear in structure, at one end provided with a phosphoramidite moiety, at an opposing end provided with a sulfhydryl, amino or hydroxyl moiety, the two ends linked through a hydrophilic spacer chain. Methods of using and synthesizing the novel reagents are disclosed as well.