CAS: 76985-10-9; Boc-D-2-Nal-Oh

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CAS号112568-12-4 安替肽 | CAS号147577-61-5 b°C-n-methyl-d-...

合成工艺路线路线简述

    (R)-N-Acetyl-3-(2-Naphthyl)Alanine Methyl Ester置于盐酸,甲烷磺酸,水,Sodium Hydroxide体系中,用 甲醇 作为反应溶剂,化学反应 100.0H,反应生成 Boc-3-(2-萘基)-D-丙氨酸
    参考文献:铑-甲基bophoz催化不对称加氢制备单一对映异构体2-萘丙氨酸衍生物
    标题:铑-甲基bophoz催化不对称加氢制备单一对映异构体2-萘丙氨酸衍生物
    摘要:2-萘基丙氨酸和的单一对映体ñ-叔由2-萘甲醛制备丁氧羰基2-萘基.该序列已优化并以多千克规模运行,关键步骤是使用甲基bophoz的铑配合物不对称氢化2-乙酰氨基-3-(2-萘基)丙酸甲酯配体,以97.9%ee的规模顺利进行.通过使2-氨基-3-(2-萘基)丙酸甲酯甲磺酸加成盐结晶(氢化产物的酸性脱酰作用的产物),可以提高至> 99.5%ee.对于这些类型的氨基酸衍生物,用于增强对映体纯度的方案似乎是通用的.随后的转化不影响对映体纯度,以> 99.5%ee提供所需产物.
    DOI:10.1021/op050026G

    海关参考信息

    专利信息


    专利号:US-9388212-B2
    优先权日:2013-02-21
    标 题:Solid phase peptide synthesis via side chain attachment
    发明人:BARLOS KLEOMENIS K
    权利人:CHEMICAL & BIOPHARMACEUTICAL LAB OF PATRAS S A
    摘要:The present application discloses peptides and peptaibols of high purity may be obtained by solid phase peptide synthesis using as the starting resin hydroxy amino acids, hydroxy amino acid amides, hydroxy amino alcohols or small peptides containing hydroxy amino acids attached to polymers through their side chain.

    专利号:US-8173770-B2
    优先权日:2001-12-29
    标 题 :Intermediates for LHRH antagonist synthesis, process for the production, and process for LHRH antagonist production
    发明人:RASMUSSEN JON H; RASMUSSEN PALLE H; WACHS WOLFGANG O; HANSEN STEFAN; FOMSGAARD JENS
    权利人:RASMUSSEN JON H; RASMUSSEN PALLE H; WACHS WOLFGANG O; HANSEN STEFAN; FOMSGAARD JENS; CARLBIOTECH LTD AS
    摘要:The peptides Ac-D-2Nal-D-4ClPhe-D-3Pal-OH and Boc-D-2Nal-D-4ClPhe-D-3Pal-OH are intermediates useful in the synthesis of LHRH analogs by coupling with suitable heptapeptides, in particular with the heptapeptides P 1 -Ser(P 2 )-MMeTry(P 3 )-D-Lys(Nic)-Leu-Lys(iPr,P 4 )-Pro-D-AlaNH 2 and P 1 -Ser(P 2 )-NMeTry(P 3 )-D-Asn-Leu-Lys(iPr,P 4 )-Pro-D-AlaNH 2 .

    专利号:US-5710247-A
    优先权日:1996-03-19
    标题:Process and intermediates for the synthesis of LHRH antagonists
    发明人:FUNK KENNETH W; LUNDELL EDWIN O; MILLER ROBERT B; CHANG JANE L; KISHORE VIMAL; NAPIER JAMES J; STAEGER MICHAEL A
    权利人:ABBOTT LAB
    摘要:A method is provided for preparing decapeptide and undecapeptide derivatives of LHRH by solution phase peptide chemistry as well as intermediate peptides useful in the same method.

    专利号:ES-2296050-T3
    优先权日:2001-12-29
    标 题:INTERMEDIATE PRODUCTS FOR SYNTHESIS OF ANTAGONISTS OF LHRH, PROCEDURE FOR ITS PRODUCTION AND PROCEDURE FOR THE PRODUCTION OF ANTAGONISTS OF LHRH.

    专利号:CN-1622954-A
    优先权日:2001-12-29
    标题:Intermediates for the synthesis of LHRH antagonists, methods for their production and methods for the production of LHRH antagonists

    专利号:SE-0104463-D0
    优先权日:2001-12-29
    标题:Intermediates for Synthesis of LHRH Antagonists, Methods of Preparation and Methods for Preparation of LHRH Antagonists
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    主要参考文献

    参考标题: Process For Preparation Of Lanreotide Acetate Procédé De Préparation D'Acétate De Lanréotide
    摘要:The Invention Relates To An Improved Method For The Solution Phase Synthesis Of Lanreotide Acetate (1) Comprising Coupling Of Two Suitably Protected Tetrapeptide Fragments Wherein The Threonine Hydroxyl Is Protected, To Give An Octapeptide, Which On Deprotection, Oxidation, Followed By Treatment With Acetic Acid Provides Lanreotide Acetate (1) Having Desired Purity.

    合成参考文献

    合成方法参考DOI号:10.1016/j.tetasy.2012.06.020
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