专利号:US-6849743-B2 优先权日:1997-08-15 标 题 :Synthesis of clasto-lactacystin β-lactone and analogs thereof 发明人:SOUCY FRANCOIS; FLAMONDON LOUIS; BEHNKE MARK; ROUSH WILLIAM 权利人:MILLENNIUM PHARM INC 摘要:The present invention is directed to an improved synthesis of clasto-lactacystin-β-lactone, and analogs thereof, that proceeds in fewer steps and in much greater overall yield than syntheses described in the prior art. The synthetic pathway relies upon a novel stereospecific synthesis of an oxazoline intermediate and a unique stereoselective addition of a formyl amide to the oxazoline. Also described are novel clasto-lactacystin-β-lactones, and analogs thereof and their use as proteasome inhibitors.
专利号:US-7183059-B2 优先权日:1998-03-23 标 题 :Synthesis of compounds and libraries of compounds 发明人:VERDINE GREGORY L; CHYTIL MILAN; DIDIUK MARY T; MALINKY TIFFANY 权利人:HARVARD COLLEGE 摘要:A method of generating a compound having at least one biological activity of a peptide. The method includes identifying a biologically active peptide, providing a first monomer which contains terminal reactive moieties and at least one functionalizable group, providing a second monomer which contains terminal reactive moieties and at least one functionalizable group, and reacting first and second monomer under stereo-and/or regiochemically controlled conditions to yield a compound in which the monomers are attached by way of terminal reactive moieties.
专利号:US-5256811-A 优先权日:1991-05-23 标 题:Certain intermediates for the preparation of neuinic acid derivatives 发明人:TODD RICHARD S; REEVE MAXWELL 权利人:BRITISH BIO TECHNOLOGY 摘要:compounds of formula I ##STR1## wherein R 1 represents a C 1-8 alkyl, C 2-8 alkenyl, C 2-8 alkynyl, C 3-8 cycloalkyl(C 1-8 )alkyl, C 1-8 hydroxyalkyl, C 1-8 alkylthio, phenyl or substituted phenyl; n R 3 represents a C 1-8 alkyl, C 2-8 alkenyl, C 2-8 alkynyl, CO2(C 1-8 )alkyl, CO 2 (C 2-8 ) alkenyl, C 1-8 alkylthio, (C 1-2 )alkyl CO 2 (C 1-8 ) alkyl or C 1-8 aldehydroalkyl where the aldehyde function is protected by a suitable protecting group (for example, an acetal such as a dimethyl acetal); n R 4 represents a hydrogen atom, C 1-8 alkyl or C 2-8 alkenyl; n Z represents a group (CH 2 ) n or a branched alkyl chain; n n is 1 to 8; n and each of a, b and c is independently a single or a double bond; n can be prepared relatively easily and in good xxx at room temperature by reacting a compound of general formula II ##STR2## wherein R 2 , R 3 , R 4 , Z, a, b and c are as define din general formula I; with a compound of general formula III n n CHI.sub.2 R.sup.1 (III) n n wherein R 1 is as defined in general formula I; n in the presence of metal ions such as chromium (II) ions. The sever conditions of the Wittig reaction can therefore be avoided. n Compounds of formula I are useful intermediates in the synthesis of mevinic acids, which are potent inhibitors of HMG-CoA reductase and which are useful in the treatment of hypocholesterolaemia an hyperlipidaemia.
专利号:US-6525096-B1 优先权日:1990-11-27 标题:GABA and L-glutamic acid analogs for antiseizure treatment 发明人:SILVERMAN RICHARD B; ANDRUSZKIEWICZ RYSZARD; YUEN PO-WAI 权利人:UNIV NORTHWESTERN; WARNER LAMBERT CO 摘要:A compound of the formulawherein R1 is a straight or branched alkyl group having from 1 to 6 carbon atoms, phenyl, or cycloalkyl having from 3 to 6 carbon atoms; R2 is hydrogen or methyl; and R3 is hydrogen, methyl or carboxyl; which is useful in the treatment of seizure disorders. Processes are disclosed for the preparation of the compound. Intermediates prepared during the synthesis of the compound are also disclosed.
专利号:WO-2023088077-A1 优先权日:2021-11-21 标题 :Biocatalysts and methods for the synthesis of pregabalin intermediates
专利号:US-2003191322-A1 优先权日:1997-08-15 标题:Synthesis of clasto-lactacystin beta-lactone and analogs thereof