专利号:US-2004018598-A1 优先权日:2000-05-30 标题 :Bio-intermediates for use in the chemical synthesis of polyketides 发明人:SANTI DANIEL; ASHLEY GARY; MYLES DAVID C 摘要:The present invention relates to compounds made by a subset of modules from one or more polyketide synthase (“PKSâ€?) genes that are used as starting material in the chemical synthesis of novel molecules, particularly naturally occurring polyketides or derivatives thereof. The biologically derived intermediates (“bio-intermediatesâ€?) generally represent particularly difficult compounds to synthesize using traditional chemical approaches due to one or more stereocenters. In one aspect of the invention, an intermediate in the synthesis of epothilone is provided that feeds into the synthetic protocol of Danishefsky and co-workers. In another aspect of the invention, intermediates in the synthesis of discodermolide are provided that feed into the synthetic protocol of Smith and co-workers. By taking advantage of the inherent stereochemical specificity of biological processes, the syntheses of key intermediates and thus the overall syntheses of compounds like epothilone and discodermolide are greaty simplified.
专利号:US-2008103312-A1 优先权日:2006-08-29 标 题:Processes for the synthesis of 5-phenyl-1-trityl-1H-tetrazole 发明人:KANSAL VINOD K; MISTRY DHIRENKUMAR N; VASOYA SANJAY L; LUNAGARIYA VIJAYKUMAR D 权利人:KANSAL VINOD K; MISTRY DHIRENKUMAR N; VASOYA SANJAY L; LUNAGARIYA VIJAYKUMAR D 摘要:Provided are processes for the synthesis of 5-phenyl-1-trityl-1H-tetrazole, an intermediate useful in the synthesis of irbesartan.
专利号:US-6350878-B1 优先权日:1998-05-18 标 题 :Intermediates for the synthesis of epothilones and methods for their preparation 发明人:ALTMANN KARL-HEINZ; BAUER ARMIN; SCHINZER DIETER 权利人:NOVARTIS AG 摘要:The invention relates to a method of synthesis for a compound of formula (I),wherein R is a heterocyclyl moiety and X1, X2, X3 and X4 are, independently of each other, protecting groups, which is appropriate for the synthesis of epothilone B and desoxyepothione B.
专利号:US-4310467-A 优先权日:1980-10-22 标题:Process and intermediates for the synthesis of vitamin D3 metabolites 发明人:BATCHO ANDREW D; BERGER JR DONALD E; USKOKOVIC MILAN R 权利人:HOFFMANN LA ROCHE 摘要:The present disclosure is directed to a process and intermediates for the synthesis of Vitamin D 3 metabolites such as 1,25-dihydroxycholecalciferol, 25-hydroxycholecalciferol and 24R,25-dihydroxycholecalciferol from 17-keto steroids via intermediates having the natural steroid configuration at the 20-position. These novel intermediates are prepared from 17-keto steroids by reaction with ethyltriphenylphosphonium halides followed by reaction with formaldehyde to form comounds having the natural steroid configuration at the 20-position and which are suitable substrates for the preparation of the aforementioned Vitamin D 3 metabolites.
专利号:US-2005043376-A1 优先权日:1996-12-03 标题:Synthesis of epothilones, intermediates thereto, analogues and uses thereof 发明人:DANISHEFSKY SAMUEL J; BERTINATO PETER; SU DAI-SHI; MENG DONGFANG; CHOU TING-CHAO; KAMENECKA TED; SORENSEN ERIK J; BALOG AARON; SAVIN KENNETH A 摘要:The present invention provides convergent processes for preparing epothilone A and B, desoxyepothilones A and B, and analogues thereof. Also provided are analogues related to epothilone A and B and intermediates useful for preparing same. The present invention further provides novel compositions based on analogues of the epothilones and methods for the treatment of cancer and cancer which has developed a multidrug-resistant phenotype.
专利号:US-5194602-A 优先权日:1988-04-08 标题 :9α-hydroxy-17-methylene steroids, process for their preparation and their use in the preparation of corticosteroids 发明人:BATISI JACOBUS N M; MARX ARTHUR F 权利人:GIST BROCADES NV 摘要:New 9α-hydroxy-17-methylene steroids are prepared by the introduction of a substituted 17-methylene group in 9α-hydroxyandrost-4-ene-3, 17-dione. n The resulting compounds are useful starting compounds in the synthesis of corticosteroids.