专利号:US-4239689-A 优先权日:1978-12-18 标题 :Total synthesis of the utero-evacuant substance d,l-zoapatanol 发明人:KANE VINAYAK V 权利人:ORTHO PHARMA CORP 摘要:A method for the synthesis of racemic 2S*, 3R*-6E-(2'-hydroxyethylidene)-2-methyl-2-(4',8'-dimethyl-5'-oxo-7'-nonenyl)-oxepan-3-ol is described. The naturally occurring product, 2S, 3R-6E-(2'-hydroxyethylidene)-2-methyl-2-(4',8'-dimethyl-5'-oxo-7'-nonenyl)-oxepan-3-ol, is one of the active components of the zoapatle plant.
专利号:US-2007082943-A1 优先权日:2005-04-01 标 题:Process for preparation of substantially pure glimepiride 发明人:KADAM SURESH M; TARUR VENKATASUBRAMANIAN R; NAIK SANJAY J; GAVHANE SACHIN B 权利人:KADAM SURESH M; TARUR VENKATASUBRAMANIAN R; NAIK SANJAY J; GAVHANE SACHIN B 摘要:The present invention discloses a novel process for purification of trans-4-methyl cyclohexylamine HCl and 4[-2-(3-Ethyl-4-methyl-2-carbonyl pyrrolidine amido) ethyl] benzene sulfonamide used in the synthesis of 3-Ethyl-2,5-dihydro-4-methyl-N-[2-[4-[[[[(trans-4-methyl cyclohexyl)amino]carbonyl]amino]sulfonyl]phenyl]ethyl]-2-oxo-1H-pyrrole-1-carboxamide (I), popularly known as Glimepiride. The present invention also discloses a novel purification of Glimepiride usingS methanolic ammonia and glacial acetic acid to obtain highly pure Glimepiride Form I (I) having the undesired cis isomer below 0.15%. Glimepiride (I) is useful in the treatment of diabetes mellitus.
专利号:US-8653282-B2 优先权日:2007-10-18 标 题:Preparation of dihydrothieno [3,2-D] pyrimidines and intermediates used therein 发明人:FRUTOS ROGELIO; KRISHNAMURTHY DHILEEPKUMAR; MULDER JASON ALAN; RODRIGUEZ SONIA; SENANAYAKE CHRIS HUGH; TAMPONE THOMAS G 权利人:FRUTOS ROGELIO; KRISHNAMURTHY DHILEEPKUMAR; MULDER JASON ALAN; RODRIGUEZ SONIA; SENANAYAKE CHRIS HUGH; TAMPONE THOMAS G; BOEHRINGER INGELHEIM INT 摘要:The invention relates to improved methods of preparing dihydrothienopyrimidines of formula 1, and intermediates thereof, (I) wherein X is SO or SO 2 , preferably SO, and wherein R A , R 1 , R 2 , R 3 , R 4 and R 5 have the meanings given in the description. The methods according to this invention are more suitable for large-scale synthesis of said compounds than prior methods because the new synthetic process avoids distillation and chromatographic purification between steps and results in a higher overall yield of the desired product.
专利号:US-2005209355-A1 优先权日:2004-03-22 标 题:[Novel Reactions and the Products of Such Reactions] 发明人:ROITMAN LIPA L 权利人:ROITMAN LIPA L 摘要:A process for the synthesis of novel compounds is described comprising reacting tetrachloroethylene with substances containing active methylene group in the presence of free radical initiators. Also, a process for grafting tetrachloroethylene is described comprising reacting these compounds with polymers containing active methylene group in the presence of free radical initiators. Furthermore, a method of conducting such reactions to high conversion is described, comprising conducting the reactions in the reflux condensate. The present invention provides a novel and high yield route for heretofore unobtainable materials.
专利号:US-2016073631-A1 优先权日:2013-03-04 标 题 :Process for the preparation of dihydropyrrole derivatives 发明人:EL QACEMI MYRIEM; SMITS HELMARS; CASSAYRE JEROME YVES; MULHOLLAND NICHOLAS PHILLIP; RENOLD PETER; GODINEAU EDOUARD; PITTERNA THOMAS 权利人:SYNGENTA PARTICIPATIONS AG; SYNGENTA LTD 摘要:The present invention provides stereoselective processes for the preparation of compounds of formula (I) n n n n n n n n n n n n wherein n P is phenyl, naphthyl, a 6-membered heteroaryl group containing one or two nitrogen atoms as ring members, or a 10-membered bicyclic heteroaryl group containing one or two nitrogen atoms as ring members, and wherein the phenyl, naphthyl and heteroaryl groups are optionally substituted; n R 1 is chlorodifluoromethyl or trifluoromethyl; n R 2 is optionally substituted aryl or optionally substituted heteroaryl; n n is 0 or 1; n including the process comprising n (a-i) reacting a compound of formula II n n n n n n n n n n n n n n n n wherein P, R 1 and R 2 are as defined for the compound of formula I; n with nitromethane in the presence a chiral catalyst to give a compound of formula III n n n n n n n n n n n n n n n n wherein P, R 1 and R 2 are as defined for the compound of formula I; and n (a-ii) reductively cyclising the compound of formula III to give the compound of formula I. n n n n n The invention also provides intermediates useful for processes for the synthesis of compounds of formula (I).
专利号:US-11286224-B2 优先权日:2017-10-13 标 题 :Synthesis of aliphatic alcohols as aroma chemicals 发明人:HICKMANN VOLKER; HINDALEKAR SHRIRANG; GUPTE NITIN; ARDEKAR SADANAND; SIEGEL WOLFGANG; SWAMINATHAN VIJAY NARAYANAN; PELZER RALF 权利人:BASF SE 摘要:The present invention relates to a method for preparing a compound of formula (I). The present invention also relates to compounds of formula (A) or a compound in the form of a stereoisomer. The present invention further relates to the use of a compound of formula (A) as aroma chemical.