专利号:US-7652137-B2 优先权日:2003-03-06 标 题:Synthesis of 5 substituted 7-azaindoles and 7-azaindolines 发明人:GRACZYK PIOTR PAWEL; KHAN AFZAL; BHATIA GURPREET SINGH 权利人:EISAI R&D MAN CO LTD 摘要:The present invention provides a novel substituted azaindoline intermediate of formula (I) and a method for its synthesis. The novel substitued azaindoline intermediate (I) is provided for use in the manufacture of 5-substituted 7-azaindolines and 5-substituted 7-azaindoles.
专利号:US-7259277-B2 优先权日:2003-07-25 标题 :Advanced route for the synthesis of cPLA2 inhibitors 发明人:WU YANZHONG; RAVEENDRATH PANOLIL 权利人:WYETH CORP 摘要:A process for making a compound of formula (I) n nin which process the compound HC≡C—(CH 2 ) n —NH 2 is reacted with the compound R 1 —SO 2 Cl to produce an intermediate compound, which intermediate compound is then reacted with the compound of formulan n nto produce the compound of formula (I), and compounds produced by the process of this invention. The terms R 1 , R 2 , R 3 , R 4 and n have the definitions set forth in the specification.
专利号:US-8071718-B2 优先权日:2004-12-22 标题:Selective radiolabeling of biomolecules 发明人:PADILLA DE JESUS OMAYRA LIZ; KOVACS ERNEST WILLIAM; GLASER MATTHIAS EBERHARD; ARSTAD ERIK; SYUD FAISAL AHMED 权利人:PADILLA DE JESUS OMAYRA LIZ; KOVACS ERNEST WILLIAM; GLASER MATTHIAS EBERHARD; ARSTAD ERIK; SYUD FAISAL AHMED; GEN ELECTRIC 摘要:Provided herein are methods for introducing fluorine atom onto a biomolecule comprising: (i) providing a linker comprising a thiol-reactive terminus and an azido/alkyne-reactive terminus; (ii) reacting the thiol-reactive terminus of the linker with a biomolecule comprising at least one thiol group or a reactive derivative thereof; and (iii) subsequently reacting the azido/alkyne-reactive terminus of the linker with a fluorine-substituted azide or alkyne respectively. Also provided are compositions and method of synthesis of bifunctional linkers and bioconjugates as well as radio-diagnostic agents comprising fluorine-labeled biomolecules.
专利号:US-2012196989-A1 优先权日:2005-02-11 标题:Synthesis of homopolymers and block copolymers 发明人:BREITENKAMP KURT; SILL KEVIN N 权利人:BREITENKAMP KURT; SILL KEVIN N; INTEZYNE TECHNOLOGIES INC 摘要:The present invention relates to the field of polymer chemistry and more particularly to homopolymers and block copolymers and methods of preparing the same.
专利号:US-7582771-B2 优先权日:2003-09-03 标题:Process for the synthesis of cPLA2 inhibitors 发明人:DEHNHARDT CHRISTOPH M; MEGATI SREENIVASULU; MICHALAK RONALD S; RAVEENDRANATH PANOLIL; REN JIANXIN; WU CHARLES C; WU YANGZHONG 权利人:WYETH CORP 摘要:A process for making the compound of formula (I) n nwherein Ac represents acetate; X represents O or CH 2 ; Y represents C 1 -C 6 alkyl; and Z is selected from the group consisting of H, halogen, CN, CHO, CF 3 , OCF 3 , OH, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, C 1 -C 6 thioalkyl, NH 2 , N(C 1 -C 6 alkyl) 2 , NH(C 1 -C 6 alkyl), NC(O)—(C 1 C 6 alkyl), and NO 2 . In his process, a compound of formula (II)n n nis reacted with hydrazine to form a primary alkylamine, and then the primary alkylamine is reacted with acetic anhydride, to produce the compound of formula (I).
专利号:US-9376400-B2 优先权日:2005-06-08 标 题:Process for the synthesis of triazoles 发明人:CHEN SHILI; LOU RONGLIANG; WU YUSHENG; ZHOU JIACHENG; HANSELMANN ROGER 权利人:MELINTA THERAPEUTICS INC 摘要:The present invention relates to processes for the preparation of triazoles. These compounds are useful as anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents.