专利号:US-7825244-B2 优先权日:2005-06-10 标题:Intermediates useful in the synthesis of alkylquinoline and alkylquinazoline kinase modulators, and related methods of synthesis 发明人:BAINDUR NAND; GAUL MICHAEL DAVID; KREUTTER KEVIN DOUGLAS; XU GUOZHANG 权利人:JANSSEN PHARMACEUTICA NV 摘要:The invention is directed to alkylquinoline and alkylquinazoline compounds of Formula C: n nwherein R 1 , R 2 , R 99 , and X are as defined herein, the use of such compounds in the synthesis of protein tyrosine kinase inhibitors, particularly inhibitors of FLT3 and/or c-kit and/or TrkB.
专利号:US-8728750-B2 优先权日:2006-09-06 标 题 :Process for preparation of optically active N-protected 3-aminopyrrolidine or optically active N-protected 3-aminopiperidine and the corresponding ketones by optical resolution of the racemic amine mixtures employing a bacterial omega-transaminase 发明人:ROBINS KAREN; BORNSCHEUER UWE; HÖHNE MATTHIAS 权利人:ROBINS KAREN; BORNSCHEUER UWE; HÖHNE MATTHIAS; LONZA AG 摘要:The present invention relates to the production of optically active amines, which can be used as intermediate products in a synthesis of for instance pharmaceutical products.
专利号:US-5567830-A 优先权日:1994-02-14 标题 :Process for synthesis of acetylenic carbinols 发明人:UPASANI RAVINDRA B 权利人:COCENSYS INC 摘要:A method for the preparation of an acetylenic alcohol by reaction of 1,2-dibromoethylene with an alkyl, aryl an heteroaryl lithium in an inert solvent, followed by reaction with a carbonyl-containing compound to give an acetylenic alcohol is disclosed.
专利号:US-8013157-B2 优先权日:2006-12-20 标题:Synthesis of unsaturated piperidines from piperidones with a silyl reagent 发明人:MANI NEELAKANDHA S; MORRILL CHRISTIE 权利人:JANSSEN PHARMACEUTICA NV 摘要:Syntheses of unsaturated piperidines from piperidones through a silyl piperidine reagent via the Shapiro reaction and palladium-catalyzed cross-coupling reactions with organo halides.
专利号:US-9551018-B2 优先权日:2006-02-13 标 题 :Process for the preparation of optically active chiral amines 发明人:ROBINS KAREN; SCHEUER UWE; HOHNE MATTHIAS 权利人:LONZA AG 摘要:The present invention relates to the production of optically pure secondary amines, which can be used as intermediate products in a synthesis of for instance pharmaceutical products.
专利号:WO-2019165981-A1 优先权日:2018-03-02 标 题:Methods for synthesizing (r)-3-phenylpiperidine or/and (s)-3-phenylpiperidine and chiral intermediates of niraparib 发明人:LIU ZHENDE; GAO HEYONG 权利人:SHANGHAI BIOBOND PHARMACEUTICAL CO LTD 摘要:The synthesis method provided by the first aspect of the invention successfully prepares the target product (R)-3-phenylpiperidine or/and (S)-3-phenylpiperidine using a N-protected 3-piperidone as a starting material. The synthesis method provided by the second aspect of the invention successfully prepares the target product (R)-3-phenylpiperidine or/and (S)-3-phenylpiperidine using the same starting raw material with the ingenious use of an organic silicon reagent. The (S)-3-phenylpiperidine can be used to synthesize the chiral intermediate α, β or γ of niraparib according to the third, the fourth or the fifth aspect of the invention, respectively. In general, the methods for synthesizing (R)-3-phenylpiperidine or/and (S)-3-phenylpiperidine and the chiral intermediates α, β and γ of niraparib significantly reduces the production cost, favoring the large-scale industrial production of niraparib.