Allyl 2,2-Dimethoxyethylcarbamate置于tris(2,2'-Bipyridine)Nickel(II) Tetrafluoroborate体系中,用 四氢呋喃 用作溶剂,以60%的收率获得氨基乙醛缩二甲醇 参考文献:New And Mild Allyl Carbamate Deprotection Method Catalyzed By Electrogenerated Nickel Complexes 标题:New And Mild Allyl Carbamate Deprotection Method Catalyzed By Electrogenerated Nickel Complexes 摘要:A Ni(II)-Catalyzed Electrochemical Procedure For The Simple And Mild Deprotection Of Allyl Carbamates To The Corresponding Amines Is Described. The Amines Are Obtained In Yields Of 40-99% And The Method Is Compatible With Several Functional Groups. Electrolyses Are Carried Out In Dmf Or In Thf In Single-Compartment Cells In The Presence Of A Consumable Zinc Anode. (C) 2000 Elsevier Science Ltd. All Rights Reserved. Doi:10.1016/s0040-4039(00)01223-5
专利号:US-7928223-B2 优先权日:2008-06-20 标题:Process for the synthesis of 7,8-dimethoxy-1,3-dihydro-2H-3-benzazepin-2-one, and application 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 the compound of formula (I): n n n n n n n n n n Application in the synthesis of ivabradine, addition salts thereof with a pharmaceutically acceptable acid and hydrates thereof.
专利号:WO-2019202611-A1 优先权日:2018-04-21 标题:An improved process for the synthesis of ivabradine and its pharmaceutically acceptable salts 发明人:NANDEPU Venkateswara Rao; BOPPANA DURGA PRASAD 权利人:METROCHEM API PVT 摘要:: Disclosed herein is an improved process for the preparation of Ivabradine and pharmaceutically acceptable salts thereof. The invention more particularly disclosesthe synthesis of key intermediates viz.,(S)-N-[(4,5-dimethoxybenzocydobut-l-yl)-methyl]-N- (methyl)amine hydrochloride of Formula-II and 3-(3-Iodopropyl)-7,8-dimethoxy-1,3-dihydro-2H-3-benzapin-2-one of Formula-III, and its use in industrial synthesis of Ivabradine and pharmaceutically acceptable salts thereof.
专利号:WO-9517903-A1 优先权日:1993-12-28 标 题:Modular design and synthesis of oxazolone-derived molecules 发明人:HOGAN JOSEPH C JR; CASEBIER DAVID; FURTH PAUL; TU CHENG 权利人:ARQULE PARTNERS L P; HOGAN JOSEPH C JR; CASEBIER DAVID; FURTH PAUL; TU CHENG 摘要:The design and synthesis of novel oxazolone-derived molecular modules and the use of the modules in the construction of new molecules and fabricated materials is disclosed. The new molecules and fabricated materials are molecular recognition agents useful in the design and synthesis of drugs, and have applications in separations and materials science.
专利号:WO-2009115333-A1 优先权日:2008-03-20 标 题:Novel synthesis of praziquantel 发明人:DOEMLING ALEXANDER 权利人:DOEMLING ALEXANDER 摘要:The present invention discloses a novel and efficient synthesis of praziquantel (I).
专利号:US-7109377-B2 优先权日:1996-10-16 标 题:Synthesis of combinatorial libraries of compounds reminiscent of natural products 发明人:SCHREIBER STUART L; SHAIR MATTHEW D; TAN DEREK S; FOLEY MICHAEL A; STOCKWELL BRENT R 权利人:HARVARD COLLEGE 摘要:The present invention provides complex compounds reminiscent of natural products and libraries thereof, as well as methods for their production. The inventive compounds and libraries of compounds are reminiscent of natural products in that they contain one or more stereocenters, and a high density and diversity of functionality. In general, the inventive libraries are synthesized from diversifiable scaffold structures, which are synthesized from readily available or easily synthesizable template structures. In certain embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from a shikimic acid based epoxyol template. In other embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from the pyridine-based template isonicotinamide. The present invention also provides a novel ortho-nitrobenzyl photolinker and a method for its synthesis. Furthermore, the present invention provides methods and kits for determining one or more biological activities of members of the inventive libraries. Additionally, the present invention provides pharmaceutical compositions containing one or more library members.
专利号:US-6310180-B1 优先权日:1993-06-21 标 题 :Method for synthesis of proteins 发明人:TAM JAMES P 权利人:UNIV VANDERBILT 摘要:A method for peptide synthesis is disclosed that requires neither protecting groups nor activation of the C-α carboxyl groups. The method comprises ligating a first molecule to a second molecule by promoting the orthogonal coupling of the molecules to each other. In an aspect of this method, an acyl-type reaction occurs between the molecules. The method contemplates the joining of molecules of variant size to each other, as well as the coupling of multiple identical molecules. The invention also covers the ligation of unprotected peptide, proteins or nonpeptide segments to prepare therapeutic products and synthetic vaccines with linear, circularized, or branched backbone structures, as well as the site-specific modification of peptides or proteins by lipidation and pegylation.