CAS: 103733-65-9; (R)-1,2,3,4-Tetrahydro-3-Isoquinolinecarboxylic Acid

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Benzyl (3R)-Methyl-1,2,3,4-Tetrahydroisoquinoline-3-Carboxylate置于sodium Hydroxide体系中,用 水 用作溶剂,化学反应 15.0H,以90%的收率获得(R)-(+)-1,2,3,4-四氢异喹啉-3-羧酸
参考文献:Efficient Synthesis Of Racemic And Enantiomerically Pure 1,2,3,4-Tetrahydroisoquinoline-3-Carboxylic Acid And Esters
标题:Efficient Synthesis Of Racemic And Enantiomerically Pure 1,2,3,4-Tetrahydroisoquinoline-3-Carboxylic Acid And Esters
摘要:在碱催化下,1,2-双(卤甲基)苯 1 A 或 B 与 2-(乙酰氨基)丙二酸二乙酯(2)发生环化反应,随后发生脱羧反应和酰胺裂解反应,制备出了外消旋和光学纯的 1,2,3,4-四氢异喹啉-3-羧酸及酯.对映体的分解是通过与(-)-薄荷醇酯化,然后柱层析分离非对映异构体混合物,或通过与扁桃酸分离苄酯的双酯盐,以及碱催化两种酯的皂化反应来实现的.
Doi:10.1055/s-1992-26325

专利信息

专利号:US-2023391818-A1
优先权日:2020-11-05
标 题:Peptide synthesis method for suppressing defect caused by diketopiperazine formation
发明人：NOMURA KENICHI; KAGE MIRAI; TAMIYA MINORU; KANAZAWA JUNICHIRO
权利人:CHUGAI PHARMACEUTICAL CO LTD
摘要:Solid-phase synthesis of a peptide has a problem that a desired elongation reaction is prevented from proceeding by diketopiperazine and a 6-membered diamine skeleton compound formed when a protective group at the N-terminal is removed. The present inventors have found that when in production of a peptide by a solid-phase method, a peptide in which an amino group at the N-terminal is protected with a protective group having an Fmoc skeleton is treated in a specific solvent with a base having a pKa of 23 or more in acetonitrile as a conjugate acid, and a peptide chain is then elongated, it is possible to solve the problem described above.

专利号:US-5587481-A
优先权日:1996-02-20
标 题:Preparation of (S)-decahydroisoquinoline-3-carboxylic acid t-butylamide
发明人：ALLEN DAVID R; JENKINS SCOTT; KLEIN LORAINE; ERICKSON ROBERT; FROEN DIANE
权利人:MONSANTO CO
摘要:Methods for preparing (S)-N-tert-butyl-1,2,3,4-tetrahydro-3-isoquinoline-carboxamide ('tic-c'), and converting tic-c to (S)-decahydroisoquinoline-3-carboxylic acid t-butylamide ('tic-d') are disclosed. The initial step in the formation of tic-c involves the phosgenation of a substituted tetrahydroisoquinoline to form an N-carboxy anhydride. Tic-d is used as an intermediate in the synthesis of known compounds having pharmaceutical activity.

专利号:US-11420997-B2
优先权日:2018-04-13
标题:Peptide synthesis method
发明人：SUZUKI HIDEAKI; MUTO SUSUMU; FUJITA SHUJI; KUBO DAISUKE
权利人:JITSUBO CO LTD
摘要:The present invention has an object of shortening the process time and reducing use of a poor solvent for solidifying a carrier (Tag)-peptide component, by removing impurities without conducting solid-liquid separation (condensation, solid-liquid separation and drying operation) of a Tag-peptide component, in an Fmoc method using a Tag for liquid phase peptide synthesis. Provided is the peptide synthesis method that includes the following steps a-d: step a: a carrier-protected amino acid, carrier-protected peptide, or a carrier-protected amino acid amide, and an N-Fmoc-protected amino acid or an N-Fmoc-protected peptide are condensed in an organic solvent or a mixed solution of organic solvents, to obtain an N-Fmoc-carrier-protected peptide, step b: a water-soluble amine is added to the reaction solution after the condensation reaction, step c: the Fmoc group is deprotected from the protected amino group in the presence of a water-soluble amine, and step d: the reaction solution is neutralized by adding an acid, and further, by adding and washing with an acidic aqueous solution, then, by liquid-liquid separation an aqueous layer is removed to obtain an organic layer.

专利号:WO-2023214577-A1
优先权日:2022-05-02
标 题 :Peptide synthesis method for suppressing defect caused by diketopiperazine formation
发明人：KAGE MIRAI; TAMIYA MINORU; KANAZAWA JUNICHIRO; NOMURA KENICHI
权利人:CHUGAI PHARMACEUTICAL CO LTD
摘要:The present invention addresses the problem of a desired elongation reaction not progressing as a result of a 6-membered cyclic amidine skeleton structure and a diketopiperazine formed when removing an N-terminated protective group during peptide synthesis. The inventors have discovered that it is possible to solve said problem during peptide production by treating a peptide protected by an N-terminated amino group in a protective group having an Fmoc skeleton by using a base which has a pKa of 23 or higher in an acetonitrile of a conjugate acid in a specific solvent, and next, performing peptide chain elongation.

专利号:CN-110776558-B
优先权日:2019-07-01
标 题:A kind of method of solid phase synthesis icatibant acetate