专利号:US-7074920-B2 优先权日:2004-04-13 标 题:Process for the synthesis of 1,3-dihydro-2H-3-benzazepin-2-one compounds, and to the application thereof in the synthesis of ivabradine and addition salts thereof with a pharmaceutically acceptable acid 发明人:LERESTIF JEAN-MICHEL; LECOUVE JEAN-PIERRE; BRIGOT DANIEL 权利人:SERVIER LAB 摘要:Process for the synthesis of compounds of formula (I): n nwherein R 1 and R 2 , which may be the same or different, each represent a linear or branched (C 1 –C 8 )alkoxy group or form, together with the carbon atom carrying them, a 1,3-dioxane, 1,3-dioxolane or 1,3-dioxepane ring.n n Application in the synthesis of ivabradine, addition salts thereof with a pharmaceutically acceptable acid, and hydrates thereof.
专利号:US-5990341-A 优先权日:1993-11-08 标 题 :Diastereoselective synthesis hydroxyethylene dipeptide isosteres 发明人:LIOTTA DENNIS C; LAGU BHARAT RAMKRISHNA 权利人:UNIV EMORY 摘要:A process for the synthesis of hydroxyethylene dipeptide isosteres from α-N,N-di(protected)amino(alkyl or substituted alkyl) methyl ketones that can be efficiently carried out on an industrial scale. The process proceeds with excellent diastereoselectivity and chemical efficiency, and can be used to prepare a wide variety of hydroxyethylene dipeptide isosteres for a variety of uses, including as HIV-1 protease inhibitors and renin inhibitors.
专利号:US-6147217-A 优先权日:1997-02-04 标题:Synthesis of terfenadine and derivatives 发明人:SENANAYAKE CHRIS HUGH; FANG QUN KEVIN; WILKINSON SCOTT HAROLD 权利人:SEPRACOR INC 摘要:Processes for preparing compounds having the general formula: ##STR1## wherein R 1a is protected carboxy, carboxy, hydroxymethyl, protected hydroxymethyl, or methyl are disclosed. Processes of the invention begin with a starting material of the general formula IV ##STR2## wherein R 1 and R 2 are as defined in the specification.
专利号:US-2010184989-A1 优先权日:2007-03-12 标 题 :De Novo Synthesis of Conjugates 发明人:RIGGS-SAUTHIER JENNIFER; DENG BO-LIANG; REN ZHONGXU; ZHANG WEN; GU XUYUAN; DUARTE FRANCO J 权利人:NEKTAR THERAPEUTICS 摘要:The invention provides methods for the preparation of small molecule drugs that are chemically modified by covalent attachment of a water-soluble oligomer obtained from a water-soluble oligomer composition. Such drugs are produced through modification of a synthetic pathway to attach the oligomer to an intermediate compound followed by completion of the synthetic path.
专利号:US-2005227962-A1 优先权日:2004-04-13 标 题 :Process for the synthesis of 1,3-dihydro-2H-3-benzazepin-2-one compounds, and to the application thereof in the synthesis of ivabradine and addition salts thereof with a pharmaceutically acceptable acid
专利号:AU-2005200860-B2 优先权日:2004-04-13 标 题 :New process for the synthesis of 1,3-dihydro-2H-3-benzepin-2-one compounds, and application in the synthesis of ivabradine and addition salts thereof with a pharmaceutically acceptable acid
[参考文献]: Nicolas Fleury-Brégeot, Et Al. Suzuki-Miyaura Cross-Coupling Of Potassium Dioxolanylethyltrifluoroborate And Aryl/heteroaryl Chlorides. Org Lett. 2013 Apr 5;15(7):1536-9.
合成参考文献
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