专利号:US-8269001-B2 优先权日:2005-10-05 标题 :Process for the synthesis of HMG-CoA reductase inhibitors 发明人:CASAR ZDENKO 权利人:CASAR ZDENKO; LEK PHARMACEUTICALS 摘要:A novel synthesis of statins uses Wittig reaction of a heterocyclic core of statin with a lactonized side chain already possessing needed stereochemistry. Any separation of diastereoisomers is performed early in the course of synthesis.
专利号:US-7858828-B2 优先权日:2008-03-26 标 题 :Process for synthesis of (3R,3'R,6'R)-lutein and its stereoisomers 发明人:KHACHIK FREDERICK; CHANG AN-NI 权利人:UNIV MARYLAND 摘要:(3R,3′R,6′R)-Lutein and (3R,3′R)-zeaxanthin are two dietary carotenoids that are present in most fruits and vegetables commonly consumed in the US. These carotenoids accumulate in the human plasma, major organs, and ocular tissues. In the past decade, numerous epidemiological and experimental studies have shown that lutein and zeaxanthin play an important role in the prevention of age-related macular degeneration (AMD) that is the leading cause of blindness in the U.S. and Western World. The invention provides a process for the synthesis of (3R,3′R,6′R)-lutein and its stereoisomers from commercially available (rac)-α-ionone by a C 15 +C 10 +C 15 coupling strategy. In addition, the present invention also provides access to the precursors of optically active carotenoids with 3-hydroxy-ε-end group that are otherwise difficult to synthesize. The process developed for the synthesis of lutein and its stereoisomers is straightforward and has potential for commercialization.
专利号:US-2007049757-A1 优先权日:2005-08-26 标题:Methods for the synthesis of substituted amino uracils 发明人:RIEGER JAYSON M; THOMPSON ROBERT 权利人:RIEGER JAYSON M; THOMPSON ROBERT 摘要:The invention provides novel methods of preparing substituted amino uracil compounds that can be employed as useful intermediates in the synthesis of various xanthines. Highly regioselective unsymmetrical amino uracils can be obtained using these methods which is a particular advantage over other existing methods.
专利号:US-4284582-A 优先权日:1978-04-28 标 题 :Process for the preparation of cyclopropane derivatives, intermediates in the synthesis of pyrethroid insecticides 发明人:KAYE ALBERT E; TUCKER ALAN C 权利人:ICI LTD 摘要:Compounds of formula: wherein both groups X are chlorine, bromine or trifluoromethyl, or one X is chlorine or bromine and the other is trifluoromethyl, and Y is -CN or -COOR in which R is an alkyl group, are obtained by (A) reacting a compound of the formula: wherein X1 is chlorine or bromine, with a compound of the formula: X2C=CH-CH=C(CH3)2 in the presence of metallic copper or at least one copper salt and a base, or (B) reacting a compound of the formula: Y-CH2-CN with a compound of the formula: X2C=CH-CH=C(CH3)2 and chlorine or bromine, in the presence of at least one reducible copper salt and a base, or (C) reacting a compound of formula: X-CH2-CN with a compound of the formula: wherein X1 is chlorine or bromine, in the presence of at least one copper salt. The compounds are intermediates in the synthesis of pyrethroid insecticides.
专利号:US-4866175-A 优先权日:1966-11-08 标 题 :Novel process for the synthesis of quinoxaline and benzimidazole-N-oxides 发明人:ISSIDORIDES COSTAS H; HADDADIN MAKHLUF J 权利人:RESEARCH CORP 摘要:The synthesis of quinoxaline and benzimidazole-N-oxides and of ester amd amide derivatives of 3-hydroxy-2-quinoxalinecarboxylic acid by a movel process consisting of the reaction between a benzofuroxan and an activated methylene-containing compound under basic conditions.
专利号:WO-2012059797-A1 优先权日:2010-11-04 标题 :Process for synthesis of (s) - pregabalin 发明人:ROY BHAIRAB NATH; SINGH GIRIJ PAL; LATHI PIYUSH SURESH; AGRAWAL MANOJ KUNJABIHARI; MITRA RANGAN; RUPNAWAR MANOJ DATTATRAYA 权利人:LUPIN LTD; ROY BHAIRAB NATH; SINGH GIRIJ PAL; LATHI PIYUSH SURESH; AGRAWAL MANOJ KUNJABIHARI; MITRA RANGAN; RUPNAWAR MANOJ DATTATRAYA 摘要:Improved process for the synthesis of (S)-pregabalin having more than 99% ee through (S) 3-cyano-5-methyl-hexanoic acid has been developed. In addition to above, a novel process for resolution of ( RS ) - 3-cyano-5-methyl-hexanoic acid through diastereomeric salt formation with cinchonidine to obtain ( S ) - 3-cyano-5-methyl-hexanoic acid in high yield and high optical purity has been developed and furthermore process for recovery/ reuse of cinchonidine is also developed to improve the overall process efficiency.
[参考文献]: Yulia Kaluzhny, Et Al. The Epiocular Eye Irritation Test (Eit) For Hazard Identification And Labelling Of Eye Irritating Chemicals: Protocol Optimisation For Solid Materials And The Results After Extended Shipment. Altern Lab Anim. 2015 May;43(2):101-27.
合成参考文献
参考文献:10.1107/s1600536811016370 摘要:Vasin VA, Bolusheva IY, Neverov VA, Somov NV. Methyl c-1-cyano-t-2-methyl-sulfonyl-3-phenyl-cyclo-propane-carboxyl-ate. Acta Crystallogr Sect E Struct Rep Online. 2011 Jun 01;67(Pt 6):o1504.