专利号:US-9481680-B2 优先权日:2014-03-20 标题 :Process for the preparation of key intermediates of omarigliptin 发明人:DE LUCCHI OTTORINO; ROSSO ENRICO; ZARAMELLA SIMONE; TARTAGGIA STEFANO 权利人:F I S —FABBRICA ITALIANA SINTETICI S P A; F I S —FABBRICA ITALIANA SINTETICI S P A 摘要:An improved process for the preparation of a key intermediate for the synthesis of the active ingredient Omarigliptin is provided. The key intermediate is a compound having the following formula (I) n nwherein R 1 is propargyl or allyl group and P is an amine protecting group. The compound of formula (I) is prepared by converting a compound of formula (IV)n n nby an amination reaction to a compound of formula (III),n n nwhich is then protected to provide a compound of formula (II),n n nwhich is then alkylated to provide the compound of formula (I).
专利号:US-7411088-B2 优先权日:2004-02-20 标 题:Stereoselective synthesis of a 4,4-disubstituted cyclohexanepropanoic acid 发明人:BRANDS KAREL MARIE JOSEPH; BREWER SARAH ELIZABETH; DAVIES ANTONY JOHN; DOLLING ULF H; HAMMOND DEBORAH CAMILLE; LIEBERMAN DAVID ROSS; SCOTT JEREMY PETER 权利人:MERCK & CO INC; MERCK SHARP & DOHME 摘要:There is provided stereoselective route to a compound of formula I: n nwherein R represents H or an alkali metal, Ar 1 represents 4-chlorophenyl and Ar 2 represents 2,5-difluorophenyl.
专利号:US-9676783-B2 优先权日:2008-10-22 标 题:Method of treatment using substituted pyrazolo[1,5-A] pyrimidine compounds 发明人:HAAS JULIA; ANDREWS STEVEN W; JIANG YUTONG; ZHANG GAN 权利人:ARRAY BIOPHARMA INC 摘要:Compounds useful in the synthesis of compounds for treating pain, cancer, inflammation, neurodegenerative disease or Typanosoma cruzi infection in a mammal.
专利号:US-7205300-B2 优先权日:1997-12-31 标 题:Aryl fused azapolycyclic compounds 发明人:COE JOTHAM WADSWORTH; BROOKS PAIGE ROANNE PALMER 权利人:PFIZER 摘要:This invention is directed to compounds of the formula (I): n nand their pharmaceutically acceptable salts, wherein R 1 , R 2 , and R 3 are as defined herein; intermediates for the synthesis of such compounds, pharmaceutical compositions containing such compounds; and methods of using such compounds in the treatment of neurological and psychological disorders.
专利号:US-2007225520-A1 优先权日:2004-02-20 标题 :Stereoselective Synthesis of a 4,4-Disubstituted Cyclohexanepropanoic Acid
专利号:CA-2556348-A1 优先权日:2004-02-20 标 题 :Stereoselective synthesis of a 4,4-disubstituted cyclohexanepropanoic acid