专利号:US-7390931-B2 优先权日:2004-04-01 标 题:Preparation of P-chirogenic phospholanes and their use in asymmetric synthesis 发明人:HOGE II GARRETT STEWART 权利人:PFIZER 摘要:Materials and methods for preparing P-chirogenic monophospholanes and bisphospholanes are disclosed. The methods employ stereoselective cyclization to generate the phospholane rings followed by pyramidal inversion to access a variety of P-chirogenic phospholanes. When bound to transition metals such as rhodium, the disclosed P-chirogenic phospholanes may be used as catalysts in asymmetric synthesis of valuable pharmaceutical chemical entities, including pregabalin.
专利号:US-2008312430-A1 优先权日:2004-10-20 标题:Method of Preparing or Synthesizing Polyazamacrocycle Derivatives 发明人:CIHELNIK SIMON; DROZ LADISLAV; SRAMEK MARTIN 权利人:THERAPHARM GMBH 摘要:The present invention relates to novel processes for the synthesis of polyazamacrocycle derivatives. Furthermore, the present invention relates to novel polyazamacrocycle derivatives as well as novel intermediates for the synthesis of said polyazamacrocycle derivatives.
专利号:US-6482851-B1 优先权日:1998-02-04 标题 :Synthesis of dysidiolide and uses thereof 发明人:DANISHEFSKY SAMUEL J; MAGNUSON STEVEN R; ROSEN NEAL; SEPP-LORENZINO LAURA 权利人:SLOAN KETTERING INST CANCER; UNIV COLUMBIA 摘要:This invention provides a process for the preparation of a racemic mixture of dysidiolide a method for inhibiting growth of cancerous cells comprising contracting an amount of the racemic mixture of dysidiolide effective to inhibit the growth of said cells. Further provided is a method for treating cancer in a subject which comprises administering to the subject a therapeutically effective amount of the racemic mixture of dysidiolide.
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-8592587-B2 优先权日:2007-03-21 标题 :Transannular rearrangement of activated lactams 发明人:MARTINEZ JEAN; DEWYNTER GEORGES; FARRAN DANIEL 权利人:MARTINEZ JEAN; DEWYNTER GEORGES; FARRAN DANIEL; CENTRE NAT RECH SCIENT; UNIV MONTPELLIER I 摘要:The disclosure relates to a method for the synthesis of a compound of the following formula (I) in which: R1 and R2 are independently an N-protective group; R3 is a hydrogen atom, a C 1 -C 6 alkyl group, a C 1 -C 6 arylalkyl group, a C 2 -C 6 alkenyl group, or a alkoxycarbonylalkyl group; Y is a —C(HR4)- group in which R4 is a hydrogen atom, a C 1 -C 6 alkyl group, an aryl group, a C 1 -C 6 arylalkyl group, or a C 2 -C 6 alkenyl group; or an orthophenylene group.
专利号:WO-2014203045-A1 优先权日:2013-06-20 标 题:A novel, green and cost effective process for synthesis of tert-butyl (3r,5s)-6-oxo-3,5-dihydroxy-3,5-o-isopropylidene-hexanoate 发明人:ROY BHAIRABNATH; SINGH GIRIJ PAL; LATHI PIYUSH SURESH; AGRAWAL MANOJ KUNJABIHARI; MITRA RANGAN; TRIVEDI ANURAG; PISE VIJAY SADASHIV; RUPANWAR MANOJ 权利人:LUPIN LTD 摘要:The present invention provides a process of preparation of an intermediate useful for the preparation of statins more particularly the present invention relates to an eco-friendly and cost effective process for the preparation of tert -butyl (3R,5S)-6-oxo-3,5-dihydroxy- 3,5-O-isopropylidene-hexanoate [I].