专利号:US-9745281-B2 优先权日:2013-02-14 标 题 :Method for the synthesis of 4-(heterocycloalkyl)-benzene-1,3,-diol compounds 发明人:BOITEAU JEAN-GUY 权利人:GALDERMA RES & DEV 摘要:A method is described for the synthesis of 4-(heterocycloalkyl)-benzene-1,3-diol compounds of general formulae (I) and (II): n nwherein X can be an oxygen atom or a sulphur atom. Also described, is a method for the synthesis of the reactive intermediates of general formula (7a) or (7b)n n nNovel compounds as synthesis intermediates are also described.
专利号:US-5567830-A 优先权日:1994-02-14 标题 :Process for synthesis of acetylenic carbinols 发明人:UPASANI RAVINDRA B 权利人:COCENSYS INC 摘要:A method for the preparation of an acetylenic alcohol by reaction of 1,2-dibromoethylene with an alkyl, aryl an heteroaryl lithium in an inert solvent, followed by reaction with a carbonyl-containing compound to give an acetylenic alcohol is disclosed.
专利号:US-8487108-B2 优先权日:2005-11-14 标题 :Piperidinyl carbamate intermediates for the synthesis of aspartic protease inhibitors 发明人:BALDWIN JOHN J; CLAREMON DAVID A; TICE COLIN; CACATIAN SALVACION; DILLARD LAWRENCE W; ISHCHENKO ALEXEY V; YUAN JING; XU ZHENRONG; MCGEEHAN GERARD; SIMPSON ROBERT D; SINGH SURESH B; ZHAO WEI; FLAHERTY PATRICK T 权利人:BALDWIN JOHN J; CLAREMON DAVID A; TICE COLIN; CACATIAN SALVACION; DILLARD LAWRENCE W; ISHCHENKO ALEXEY V; YUAN JING; XU ZHENRONG; MCGEEHAN GERARD; SIMPSON ROBERT D; SINGH SURESH B; ZHAO WEI; FLAHERTY PATRICK T; VITAE PHARMACEUTICALS INC 摘要:The present invention is directed to aspartic protease inhibitors. Certain aspartic protease inhibitors of the invention can be represented by the following structural formula or a pharmaceutically acceptable salt thereof. The present invention is also directed to pharmaceutical compositions comprising the disclosed aspartic protease inhibitors. The present invention is further directed to methods of antagonizing one or more aspartic proteases in a subject in need thereof, and methods for treating an aspartic protease mediated disorder in a subject using the disclosed aspartic protease inhibitors.
专利号:US-9527855-B2 优先权日:2011-06-29 标题:Process for preparing chiral dipeptidyl peptidase-IV inhibitors 发明人:ZACUTO MICHAEL J; DUNN ROBERT F; MOMENT AARON J; JANEY JACOB M; LIEBERMAN DAVID; SHEEN FAYE; BREMEYER NADINE; SCOTT JEREMY; KUETHE JEFFREY T; TAN LUSHI; CHEN QINGHAO 权利人:MERCK SHARP & DOHME; MERCK SHARP & DOHME 摘要:A process for the preparation of pyrazolopyrolidines of structural formula I: n nand W isn n nor P, wherein in P is an amine protecting group. These compounds are useful in the synthesis of dipeptidyl peptidase-IV inhibitors for the treatment of Type 2 diabetes. Also provided are useful intermediates obtained from the process.
专利号:US-7902376-B2 优先权日:2008-01-23 标 题 :Process for preparing chiral dipeptidyl peptidase-IV inhibitor intermediates 发明人:XU FENG; KIM MARY M; KOHMURA YOSHINORI; SLADICKA TRICIA; ROSEN JONATHAN D; ZACUTO MICHAEL J 权利人:MERCK SHARP & DOHME; BANYU PHARMA CO LTD 摘要:A novel process is provided for the preparation of chiral trans-2,3-disubstituted 5-oxotetrahydropyrans of structural formula (I): n nwherein Ar is optionally substituted phenyl and P is a primary amine protecting group. These compounds are useful in the synthesis of dipeptidyl peptidase-IV inhibitors for the treatment of Type 2 diabetes. Also provided are useful intermediates obtained from the process.
专利号:US-2016185749-A1 优先权日:2013-02-14 标题:Method for the synthesis of 4-(heterocycloalkyl)-benzene-1,3,-diol compounds
摘要:Zhang, J., Science of Synthesis Knowledge Updates, (2010) 4, 250. 摘要:Mukherjee, S., Science of Synthesis: Asymmetric Organocatalysis, (2012) 1, 236. 摘要:Faisca Phillips, A. M.; Guedes da Silva, M. F. C.; Pombeiro, A. J. L., Science of Synthesis: Cross-Dehydrogenative Coupling, (2023) nan, 607.