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-8513429-B2 优先权日:2002-08-23 标 题:Synthesis of epothilones, intermediates thereto and analogues thereof 发明人:DANISHEFSKY SAMUEL J; RIVKIN ALEXEY; FUMIKIKO YOSHIMURA; CHOU TING-CHAO; GABARDA ANA E; DONG HUAJIN 权利人:DANISHEFSKY SAMUEL J; RIVKIN ALEXEY; FUMIKIKO YOSHIMURA; CHOU TING-CHAO; GABARDA ANA E; DONG HUAJIN; SLOAN KETTERING INSITUTE FOR CANCER RES 摘要:The present invention provides compounds of formula (I): n n n n n n n n n n n n as described generally and in classes and subclasses herein. The present invention additionally provides pharmaceutical compositions comprising compounds of formula (I) and provides methods of treating cancer comprising administering a compound of formula (I).
专利号:US-7875638-B2 优先权日:2002-08-23 标题:Synthesis of epothilones, intermediates thereto, analogues and uses thereof 发明人:DANISHEFSKY SAMUEL J; RIVKIN ALEXEY; YOSHIMURA FUMIHIKO; CHOU TING-CHAO; GABARDA ANA E; DONG HUAJIN; WU KAIDA; MOORE MALCOLM A S; DORN DAVID 权利人:SLOAN KETTERING INST CANCER 摘要:The present invention provides compounds of formula (I): n n n n n n n n n n n n as described generally and in classes and subclasses herein. The present invention additionally provides pharmaceutical compositions comprising compounds of formula (I) and provides methods of treating cancer comprising administering a compound of formula (I).
专利号:US-8030503-B2 优先权日:2007-05-11 标题:Process for the preparation of epothilones 发明人:CHEN YUE; LI YONG 权利人:KOSAN BIOSCIENCES INC 摘要:Intermediates in the preparation of epothilones and epothilone analogs are provided along with synthetic methods useful in the synthesis of epothilone compounds.
专利号:US-7884128-B2 优先权日:2005-10-13 标题:Process for total synthesis of pladienolide B and pladienolide D 发明人:KANADA REGINA MIKIE; ITO DAISUKE; SAKAI TAKASHI; ASAI NAOKI; KOTAKE YOSHIHIKO; NIIJIMA JUN 权利人:EISAI R&D MAN CO LTD 摘要:Process for producing compound of Formula: n nwherein P 2 , P 3 and R 2 are the same as defined below, characterized by comprising reacting a compound represented by Formula (7):n n nwherein P 3 means a protecting group for hydroxy group; and Het means a 1-phenyl-1H-tetrazol-5-yl group, with a compound represented by Formula (8):n n nwherein P 2 means a protecting group for hydroxy group; and R 2 means a phenyl group which may be substituted, in the presence of a base.
专利号:US-2003176368-A1 优先权日:2001-09-06 标题:Synthesis of epothilones, intermediates thereto and analogues thereof 发明人:DANISHEFSKY SAMUEL J; BISWAS KAUSTAV; CHAPPELL MARK; LIN HONG; NJARDARSON JON T; LEE CHUL BOM; RIVKIN ALEXY; CHOU TING-CHAO 摘要:The present invention provides compounds of formula (I): n n n as described generally and in classes and subclasses herein. The present invention additionally provides pharmaceutical compositions comprising compounds of formula (I) and provides methods of treating cancer comprising administering a compound of formula (I).