专利号:US-7323575-B2 优先权日:2003-04-09 标题:Process for the synthesis of (2S)-indoline-2-carboxylic acid 发明人:SOUVIE JEAN-CLAUDE; LECOUVE JEAN-PIERRE 权利人:SERVIER LAB 摘要:Process for the synthesis of (2S)-indoline-2-carboxylic acid of formula (I): n nApplication in the synthesis of perindopril and its pharmaceutically acceptable salts.
专利号:US-9126995-B2 优先权日:2011-11-08 标题:Method for catalytic asymmetric synthesis of optically active isoxazoline compound and optically active isoxazoline compound 发明人:TOYAMA KEN-ICHI; MORIYAMA YUJI; MATOBA KAZUTAKA; YAOSAKA MANABU; IKEDA EITATSU 权利人:NISSAN CHEMICAL IND LTD 摘要:There is provided a method for catalytic asymmetric synthesis of optically active isoxazoline compound and an optically active isoxazoline compound. A method for catalytic asymmetric synthesis of optically active isoxazoline compound of a formula (6) including reacting an α,β-unsaturated carbonyl compound of a formula (1) and a hydroxylamine in a solvent in the presence of a base by adding a chiral phase transfer catalyst. An optically active isoxazoline compound of a formula (13) that can be synthesized by the method.
专利号:US-6555686-B2 优先权日:2000-03-23 标题:Asymmetric synthesis of quinazolin-2-ones useful as HIV reverse transcriptase inhibitors 发明人:PARSONS RODNEY L; DOROW ROBERTA L; DAVULCU AKIN H; FORTUNAK JOSEPH M; HARRIS GREGORY D; KAUFFMAN GOSS S; NUGENT WILLIAM A; RADESCA LILIAN A 权利人:BRISTOL MYERS SQUIBB PHARMA 摘要:This invention relates generally to the asymmetric synthesis of quinazolin-2-ones that are useful as inhibitors of HIV reverse transcriptase. The synthesis is accomplished through the chiral ligand mediated addition of cyclopropylacetylide.
专利号:US-4190579-A 优先权日:1977-12-29 标题:Synthesis of beta-lactams from azetidine carboxylic acid esters 发明人:LIPSHUTZ BRUCE H; WASSERMAN HARRY H; WU JAMES S 权利人:RESEARCH CORP 摘要:Azetidine carboxylic acid esters are converted into enol silyl ethers which, as enamino ketene acetals, undergo ready oxidative cleavage of the ethylenically unsaturated double bond, e.g. by dye-sensitized photo-oxygenation, to form beta-lactams. The beta-lactams and substitution products thereof are useful intermediates in the synthesis of biologically active lactams.
专利号:US-8283502-B2 优先权日:2009-04-09 标题:Autocatalytic process for the synthesis of chiral propargylic alcohols 发明人:CHINKOV NICKA; WARM ALEKSANDER; CARREIRA ERICK 权利人:CHINKOV NICKA; WARM ALEKSANDER; CARREIRA ERICK; LONZA AG 摘要:An autocatalytic process for the synthesis of chiral propargylic alcohols.
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.
1: Deka J, Satyanarayana L, Karunakar GV, Bhattacharyya PK, Bania KK. Chiral modification of copper exchanged zeolite-Y with cinchonidine and its application in the asymmetric Henry reaction. Dalton Trans. 2015 Dec 28;44(48):20949-63. doi: 10.1039/c5dt03630e. Epub 2015 Nov 18. doi: 10.1016/j.saa.2013.04.032. Epub 2013 Apr 11. doi: 10.1016/j.bbrc.2010.12.084. Epub 2010 Dec 23. doi: 10.1002/chir.22046. Epub 2012 May 10. doi: 10.1002/chem.201303261. Epub 2013 Dec 30. doi: 10.1124/dmd.109.030064. Epub 2009 Nov 12. doi: 10.1107/S0108270111027272. Epub 2011 Aug 5. doi: 10.1002/chem.200902517. doi: 10.1021/ja2054918. Epub 2011 Nov 15. doi: 10.1016/j.talanta.2009.10.011. Epub 2009 Oct 14. doi: 10.1039/c2dt12390h. Epub 2012 Mar 27. doi: 10.1021/acs.joc.5b01491. Epub 2015 Aug 12. Epub 2006 Feb 17.
合成参考文献
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