专利号:US-2010312013-A1 优先权日:2009-06-03 标 题:Steroselective synthesis of certain trifluoromethyl-substituted alcohols 发明人:FANDRICK DANIEL R; YEE NATHAN K; SONG JINHUA J; REEVES JONATHAN T 权利人:BOEHRINGER INGELHEIM INT 摘要:A process for synthesis of a compound of Formula (X) n n n n n n n n n n wherein:n R 1 is an aryl group substituted with one to three substituent groups,n wherein each substituent group of R 1 is independently C 1 -C 5 alkyl, aminocarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl, halogen, carboxy, cyano, or trifluoromethyl,n wherein each substituent group of R 1 is optionally independently substituted with one to three substituents selected from C 1 -C 3 alkyl, C 1 -C 3 alkoxy, phenyl, and alkoxyphenyl; and n n R 2 and R 3 are each independently C 1 -C 5 alkyl.
专利号:US-6822093-B2 优先权日:2000-05-23 标题 :Synthesis of heteroarylamine intermediate compounds 发明人:SONG JINHUA J; YEE NATHAN K 权利人:BOEHRINGER INGELHEIM PHARMA 摘要:Disclosed are novel 2-(5-halopyridyl) and 2-(5-halopyrimidinyl) magnesium halides, processes of making and their use in the efficient synthesis in their respective 5-halo-2-substituted pyridines and pyrimidines.
专利号:US-11466046-B2 优先权日:2014-10-08 标题 :14-membered ketolides and methods of their preparation and use 发明人:MYERS ANDREW G; SEIPLE IAN BASS; ZHANG ZIYANG 权利人:HARVARD COLLEGE 摘要:Provided herein are methods of preparing new 14-membered ketolides via coupling of an eastern and western half moiety, followed by macrocyclization, and optional functionalization. Intermediates in the synthesis of these ketolides including the eastern and western halves are also provided. Pharmaceutical compositions and methods of treating infectious diseases and inflammatory conditions using these ketolides are also provided.
专利号:US-6340751-B1 优先权日:1998-07-24 标 题 :Process for the preparation of 4-substituted azetidinone derivatives 发明人:SAITO TAKAO; MURAYAMA TOSHIYUKI; MATSUMOTO TAKAJI; MIURA TAKASHI 权利人:TAKASAGO PERFUMERY CO LTD 摘要:Disclosed is a process for the preparation of a 4-substituted azetidinone derivative, which comprises reacting an azetidinone derivative and an amide compound in the presence of a magnesium compound such as those represented by the following formulas (II): n and (IV): n represented by the following formula (III): n n n MgR 5 R 6   (III) n n n wherein R 5 represents a C 1-12 alkyl group, a C 2-5 alkenyl group, a 5- to 8-membered alicyclic group which may be substituted by a lower C 1-4 alkyl group, a phenyl group which may be substituted by a lower C 1-4 alkyl group, a lower C 1-4 alkoxy group or a halogen atom or a benzyl group which may be substituted by a lower C 1-4 alkyl group, a lower C 1-4 alkoxy group or a halogen atom, and R 6 represents a halogen atom, a methanesulfonyloxy group, a benzenesulfonyloxy group, a p-toluenesulfonyloxy group, a trifluoromethanesulfonyloxy group, an acetoxy group which may be substituted by a halogen atom or a cyano group or an OR 7 group (R 7 representing a lower C 1-4 alkyl group, a substituted or unsubstituted phenyl group or a substituted or unsubstituted benzyl group). The process provides an industrially excellent process for the preparation of a 4-substituted azetidinone derivative which permits the selective preparation of an intermediate for the synthesis of a carbapenem antibacterial agent having a desired 1-β′ configuration.
专利号:US-2007173517-A1 优先权日:2006-01-20 标 题:Synthesis of 6,7-Dihydro-5H-imidazo[1,2-a]imidazole-3-sulfonic acid amides 发明人:WIRTH THOMAS; KROEBER JUTTA; NICOLA THOMAS; RAPP ARMIN; GUTHEIL DIETER; ORLICH SIMONE A; WANG XIAO-JUN; KRISHNAMURTHY DHILEEPKUMAR 权利人:WIRTH THOMAS; KROEBER JUTTA; NICOLA THOMAS; RAPP ARMIN; GUTHEIL DIETER; ORLICH SIMONE A; WANG XIAO-JUN; KRISHNAMURTHY DHILEEPKUMAR 摘要:Disclosed is an improved multi-step process for preparing a compound of Formula I: n n nwherein R 1 to R 3 are as defined herein. The compounds of formula I inhibit the binding of human intercellular adhesion molecules to the Leukointegrins. As a result, these compounds are useful in the treatment of inflammatory and immune cell-mediated diseases.
专利号:US-7470795-B2 优先权日:2004-07-27 标 题:Synthesis of 6,7-dihydro-5H-imidazo[1,2-a]imidazole-3-sulfonic acid amides 发明人:WANG XIAO-JUN; WIRTH THOMAS; NICOLA THOMAS; ZHANG LI; FRUTOS ROGELIO PEREZ; XU YIBO; KRISHNAMURTHY DHILEEPKUMAR; NUMMY LAURENCE JOHN; VARSOLONA RICHARD J; SENANAYAKE CHRIS HUGH; KROEBER JUTTA; REEVES DIANA 权利人:BOEHRINGER INGELHEIM PHARMA; BOEHRINGER INGELHEIM INT 摘要:Disclosed is a multi-step process for preparing a compound of Formula I: n nwherein R 1 to R 3 are as defined herein. The compounds of formula I inhibit the binding of human intercellular adhesion molecules to the Leukointegrins. As a result, these compounds are useful in the treatment of inflammatory and immune cell-mediated diseases.
摘要:Micalizio, G. C., Science of Synthesis Knowledge Updates, (2012) 4, 53. 摘要:Micalizio, G. C., Science of Synthesis Knowledge Updates, (2012) 4, 62. 摘要:Bertus, P.; Boeda, F.; Pearson-Long, M. S. M., Science of Synthesis Knowledge Updates, (2012) 1, 31. 摘要:Bertus, P.; Boeda, F.; Pearson-Long, M. S. M., Science of Synthesis Knowledge Updates, (2012) 1, 32. 摘要:Bertus, P.; Boeda, F.; Pearson-Long, M. S. M., Science of Synthesis Knowledge Updates, (2012) 1, 35.