专利号:WO-8800592-A1 优先权日:1986-07-18 标题:DIASTEROSELECTIVE STRECKER SYNTHESIS OF alpha-AMINOACIDS FROM GLYCOSYLAMINE DERIVATES 发明人:KUNZ HORST; SAGER WILFRIED; PFRENGE WALDEMAR; DECKER MATHIAS 权利人:CELAMERCK GMBH & CO KG 摘要:O-acyl-protected glycosylamines, in particular 2,3,4,6-tetra-O-pivaloyl-beta-D-galactopyranosylamine (1), their preparation and their use for the diastereoselective synthesis of alpha-aminoacids. With compounds such as (1), one can obtain by Strecker synthesis high yields and high diastereomer surplus. The direction of the asymmetric induction can be determined by the selection of the solvent. This type of synthesis is particularly effective when carried with Lewis acid catalysts. One obtains also high yields and high diastereoselectivity during Ugi four component synthesis facilitated by Lewis acids by using amines such as (1).
专利号:US-8436206-B2 优先权日:2007-08-03 标 题:Process for the synthesis of (7-methoxy-1-naphthyl) acetonitrile and application in the synthesis of agomelatine 发明人:DUBUFFET THIERRY; LECOUVE JEAN-PIERRE; HERMET JEAN-PAUL 权利人:DUBUFFET THIERRY; LECOUVE JEAN-PIERRE; HERMET JEAN-PAUL; SERVIER LAB 摘要:Process for the industrial synthesis of the compound of formula (I) n nApplication of such process in the synthesis of agomelatine.
专利号:US-2012203004-A1 优先权日:2009-08-13 标题 :process for the synthesis of alkyl/aralkyl (2s)-2-(tert-butoxycarbonyl)-amino-2-[-8-azabicyclo[3.2.1]oct-3-yl]-exo-acetate and analogs thereof: key intermediates for the preparation of dppiv inhibitors 发明人:ROY BHAIRAB NATH; KAMBOJ RAJENDER KUMAR; GOERGE SHAJI K; VENUGOPAL SPINVIN C; SHANMUGVADIVELU MUTHU KUMARAN; SINHA NEELIMA 权利人:ROY BHAIRAB NATH; KAMBOJ RAJENDER KUMAR; GOERGE SHAJI K; VENUGOPAL SPINVIN C; SHANMUGVADIVELU MUTHU KUMARAN; SINHA NEELIMA; LUPIN LTD 摘要:An improved process for the synthesis of intermediates like Alkyl/Aralkyl (2S)-2-(tert-butoxycarbonyl)-amino-2-[-8-azabicyclo[3.2.1]oct-3-yl]-exo-acetate and analogs thereof which are useful in the synthesis of Dipeptidyl peptidase-IV (DP-PIV) inhibitors.
专利号:US-5338851-A 优先权日:1993-03-31 标 题:Synthesis of cis-decahydroisoquinoline-3-carboxylic acids 发明人:HUFF BRET E; KHAU VIEN V; MARTINELLI MICHAEL J; PETERSON BARRY C 权利人:LILLY CO ELI 摘要:This invention provides a process for the synthesis of cis-decahydroisoquinoline-3-carboxylic acids and provides intermediates in the synthesis thereof.
专利号:US-2023286918-A1 优先权日:2020-07-02 标 题:Manufacturing process for 3,5-dichloropicolinonitrile for synthesis of vadadustat 发明人:JURKAUSKAS VALDAS; JUNG YOUNG CHUN; KWON TAESOO; KANNAN ARUNACHALAM; GONDI VIJAYA BHASKER 权利人:AKEBIA THERAPEUTICS INC 摘要:Disclosed herein are methods and processes of preparing vadadustat or a pharmaceutically acceptable salts thereof, and intermediates (e.g., a compound of Formula (I), (I-F), (II), or (IV), or a pharmaceutically acceptable salts thereof) useful for the synthesis of vadadustat.
专利号:US-2006167025-A1 优先权日:2004-12-22 标 题:Tricyclic amino alcohols, processes for synthesis of same and use of same as anti-inflammatory drugs 发明人:BERGER MARKUS; SCHMEES NORBERT; SCHAECKE HEIKE; BAURLE STEFAN; REHWINKEL HARTMUT; MENGEL ANNE; KROLIKIEWICZ KONRAD; GROSSBACH DANJA; VOIGTLAENDER DAVID 权利人:BERGER MARKUS; SCHMEES NORBERT; SCHAECKE HEIKE; BAURLE STEFAN; REHWINKEL HARTMUT; MENGEL ANNE; KROLIKIEWICZ KONRAD; GROSSBACH DANJA; VOIGTLAENDER DAVID 摘要:The invention relates to tricyclic amino alcohols of general formula (I) n nmethod for synthesis of same and use of same as anti-inflammatory agents.
[参考文献]: G K Surya Prakash, Et Al. Effect Of Carbonates/phosphates As Nucleophilic Catalysts In Dimethylformamide For Efficient Cyanosilylation Of Aldehydes And Ketones. Proc Natl Acad Sci U S A. 2007 Feb 27;104(9):3026-30. [参考文献]: Guang-Wu Zhang, Et Al. Brnsted Acid-Catalyzed Efficient Strecker Reaction Of Ketones, Amines And Trimethylsilyl Cyanide. Org Biomol Chem. 2010 Mar 21;8(6):1399-405. [参考文献]: Jun Wang, Et Al. Asymmetric Activation Of Tropos 2,2'-Biphenol With Cinchonine Generates An Effective Catalyst For The Asymmetric Strecker Reaction Of N-Tosyl-Protected Aldimines And Ketoimines. Angew Chem Int Ed Engl. 2007;46(44):8468-70. [参考文献]: Ke Shen, Et Al. Facile And Efficient Enantioselective Strecker Reaction Of Ketimines By Chiral Sodium Phosphate. Chemistry. 2009 Jun 8;15(24):6008-14. [参考文献]: Mikhail D Kosobokov, Et Al. Difluoro(Trimethylsilyl)Acetonitrile: Synthesis And Fluoroalkylation Reactions. J Org Chem. 2012 Jul 6;77(13):5850-5.
合成参考文献
摘要:Nishimoto, Y.; Yasuda, M.; Baba, A., Science of Synthesis Knowledge Updates, (2017) 1, 203. 摘要:Nishimoto, Y.; Yasuda, M.; Baba, A., Science of Synthesis Knowledge Updates, (2017) 1, 208. 摘要:Davies, G. H. M.; Wisniewski, S. R., Science of Synthesis Knowledge Updates, (2021) 2, 147. 摘要:Nishimoto, Y.; Yasuda, M.; Baba, A., Science of Synthesis Knowledge Updates, (2017) 1, 210. 摘要:Araki, S.; Hirashita, T., Science of Synthesis Knowledge Updates, (2010) 4, 171.