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-7692019-B2 优先权日:2000-12-04 标 题:Methods for the stereoselective synthesis of substituted piperidines 发明人:AQUILA BRIAN M; BANNISTER THOMAS D; CUNY GREGORY D; HAUSKE JAMES R; HEFFERNAN MICHELE L R; HOEMANN MICHAEL Z; KESSLER DONALD W; SHAO LIMING; WU XINHE; XIE ROGER L 权利人:SEPRACOR INC 摘要:One aspect of the present invention relates to methods of synthesizing substituted piperidines. A second aspect of the present invention relates to stereoselective methods of synthesizing substituted piperidines. The methods of the present invention will find use in the synthesis of compounds useful for treatment of numerous ailments, conditions and diseases that afflict mammals, including but not limited to addiction and pain. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the substituted piperidines using the methods of the present invention. An additional aspect of the present invention relates to enantiomerically substituted pyrrolidines, piperidines, and azepines.
专利号:US-6867305-B2 优先权日:1996-12-03 标题:Synthesis of epothilones, intermediates thereto and analogues thereof 发明人:DANISHEFSKY SAMUEL J; STACHEL SHAWN J; LEE CHUL BOM; CHAPPELL MARK D; WU ZHICAL 权利人:SLOAN KETTERING INST CANCER; UNIV COLUMBIA 摘要:The present invention provides convergent processes for preparing epothilones, desoxyepothilones, and analogues thereof. The present invention further provides novel compositions and methods for the treatment of cancer and additionally provides methods for the treatment of cancer which has developed a multi-drug phenotype.
专利号:US-2002052028-A1 优先权日:2000-08-09 标题:Bio-intermediates for use in the chemical synthesis of polyketides
专利号:US-2002058817-A1 优先权日:1996-12-03 标题 :Synthesis of epothilones, intermediates thereto and analogues thereof