专利号:WO-03031376-A1 优先权日:2001-10-12 标 题 :Solid phase synthesis of substituted 1,5-benzodiazepine-2-one and 1,5-benzothiazepine-2-one 发明人:MORTON GEORGE C; SALVINO JOSEPH M; LABAUDINIERE RICHARD F; HERPIN TIMOTHY F 权利人:AVENTIS PHARMA INC; MORTON GEORGE C; SALVINO JOSEPH M; LABAUDINIERE RICHARD F; HERPIN TIMOTHY F 摘要:A solid phase synthetic method for making substituted 1,5-benzodiazepine-2-one or 1,5-benzothiazepine-2-one. The method is useful for synthesis of large numbers of compounds through automated parallel synthesis or combinatorial library generation and is thus important to rapid discovery or new therapeutic agents containing the base structure of 1,5-benzodiazepine-2-one or 1,5-benzothiazepine-2-one.
专利号:US-7138526-B1 优先权日:1999-06-15 标 题 :Solid phase synthesis of n,n-disubstituted diazacycloalkylcarboxy derivatives 发明人:HERPIN TIMOTHY F; MORTON GEORGE C; SALVINO JOSEPH M 权利人:AVENTIS PHARMA INC 摘要:A method for the solid phase synthesis of N,N-disubstituted diazacycloalkylcarboxy derivatives of general formula (I) and (II) is claimed. Examples include piperazine-2-carboxamide. The method is applicable to the synthesis or large combinatorial libraries
专利号:US-11603382-B2 优先权日:2015-12-11 标题 :Diastereoselective synthesis of phosphate derivatives 发明人:KOTALA MANI BUSHAN; DAMMALAPATI VENKATA LAKSHMI NARASIMHA RAO 权利人:NuCana plc 摘要:The present invention provides a method for the preparation of intermediates useful in the synthesis of gemcitabine-[phenyl-benzoxy-L-alaninyl)]-phosphate. It also provides a method of preparing gemcitabine-[phenyl-benzoxy-L-alaninyl)]-phosphate.
专利号:US-6127515-A 优先权日:1997-11-18 标 题:Functionalized resin for the synthesis of amides and peptides 发明人:MANFRE FRANCO; VANASSE BENOIT J; LABAUDINIERE RICHARD F; MORTON GEORGE C 权利人:AVENTIS PHARM PROD INC 摘要:This invention is directed to a functionalized amino resin of formula ##STR1## wherein S is a solid support; R is H or alkyl; A is ##STR2## Y is OH or OCOR 1 ; and R 1 is aliphatic or aromatic which is useful for the solid phase synthesis of amides, peptides and hydroxamic acids.
专利号:US-6133409-A 优先权日:1996-12-19 标 题:Process for the solid phase synthesis of aldehyde, ketone, oxime, amine, hydroxamic acid and αβ-unsaturated carboxylic acid and aldehyde compounds 发明人:SALVINO JOSEPH M; MORTON GEORGE C; MASON HELEN J; LABAUDINIERE RICHARD F 权利人:AVENTIS PHARM PROD INC 摘要:This invention is directed to a process for the solid phase synthesis of aldehyde, ketone, oxime, amine, hydroxamic acid and alpha , beta -unsaturated carboxylic acid and aldehyde compounds and to polymeric hydroxylamine resin compounds useful therefor.
专利号:US-7368568-B2 优先权日:2001-08-03 标 题 :Protected 3,5-dihydroxy-2,2-dimethyl-valeroamides for the synthesis of epothilones and derivatives and process for production and the use 发明人:WESTERMANN JURGEN; PLATZEK JOHANNES; PETROV ORLIN 权利人:BAYER SCHERING PHARMA AG 摘要:The invention relates to new protected 3,5-dihydroxy-2,2-dimethyl-valeroarnides for the synthesis of edothilones and derivatives and process for the production and the use of the new compounds for the production of epothilones or epothilone derivatives.