专利号:US-9938297-B2 优先权日:2014-08-04 标 题:Process for the synthesis of everolimus and intermediates thereof 发明人:RAO DHARMARAJ RAMACHANDRA; MALHOTRA GEENA; PULLELA VENKATA SRINIVAS; ACHARYA VINOD PARAMESHWARAN 权利人:CIPLA LTD; CIPIA LTD 摘要:The present invention relates to a novel process for the synthesis of everolimus of formula (I): n nand intermediates thereof.
专利号:US-10308665-B2 优先权日:2015-06-23 标题 :Method for the synthesis of rapamycin derivatives 发明人:ZABUDKIN OLEKSANDR; SCHICKANEDER CHRISTIAN; MATVIIENKO IAROSLAV; SYPCHENKO VOLODYMYR 权利人:SYNBIAS PHARMA AG 摘要:The present invention relates to a method for the production of a rapamycin derivative of formula (I), the method comprising the preparation of a 2-(tri-substituted silyl)oxyethyl triflate by reacting ethylene oxide and a tri-substituted silyl triflate, reaction of the resulting 2-(tri-substituted silyl)oxyethyl triflate with rapamycin in the presence of a molar excess of organic base, and deprotection to obtain the rapamycin derivative of compound (I).
专利号:US-6277983-B1 优先权日:2000-09-27 标 题:Regioselective synthesis of rapamycin derivatives 发明人:SHAW CHIA-CHENG; SELLSTEDT JOHN; NOURELDIN RAZZAK; CHEAL GLORIA K; FORTIER GENEVIEVE 权利人:AMERICAN HOME PROD 摘要:This invention provides a regioselective process for preparing a 42-ester or ether of rapamycin, and 31-silyl ether intermediates.
专利号:EP-1216251-B1 优先权日:1999-09-29 标题 :Regioselective synthesis of rapamycin derivatives 发明人:SHAW CHIA-CHENG; SELLSTEDT JOHN HAMILTON; NOURELDIN RAZZAK; CHEAL GLORIA KAREN; FORTIER GENEVIEVE 权利人:WYETH CORP 摘要:This invention provides a regioselective process for preparing a 42-ester or ether of rapamycin, and 31-silyl ether intermediates.
专利号:US-2019010168-A1 优先权日:2015-06-23 标题:Method for the synthesis of rapamycin derivatives
专利号:US-9079921-B2 优先权日:2010-11-19 标题 :Processes for preparation of Everolimus and intermediates thereof 发明人:VENKATA SRINIVAS PULLELA; EKAMBARAM GANESH; KOTHAKONDA KIRAN KUMAR; PRASAD ANEGONDI SREENIVASA 权利人:VENKATA SRINIVAS PULLELA; EKAMBARAM GANESH; KOTHAKONDA KIRAN KUMAR; PRASAD ANEGONDI SREENIVASA; BIOCON LTD 摘要:The present disclosure discloses processes of Everolimus and intermediates: reacting Sirolimus (Rapamycin) under solvent free conditions with appropriate side chain implying portion wise additions, one pot conversion, and resin mediated synthesis.