CAS: 13921-90-9; (R)-3-Amino-3-Phenylpropanoic Acid

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N-(R)-α-Methylbenzyl-(S)-3-phenylisoxazolidin-5-one N-(phenylacetyl)-3-amino-3-phenylpropanoic acid tert-butyl (R)-3-amino-3-phenylpropionate 4-phenylazetidin-2-one (R)-3-dimethylamino-3-phenylpropionic acid (R)-3-benzamido-3-phenylpropanoic acid (R)-3-[4-((R)-2-Carboxy-1-phenyl-ethylcarbamoyl)-pyridine-2-sulfonylamino]-3-phenyl-propionic acid (R)-3-benzamido-3-phenylpropanoic acid methyl ester

合成工艺路线路线简述

    Dl-苯丙氨酸置于alanine Racemase (Accession Number Ae015451 Range 4,245,041-4,246,270),Cloned From The Genome Of Pseudomonas Putida (Kt2440),Taxus Phenylalanine Aminomutase Enzyme体系中,用 水,甘油 用作溶剂,化学反应 20.0H,反应生成(R)-3-氨基-3-苯基丙酸
    参考文献:通过消旋酶/氨基酸突变酶催化,外消旋α-芳基丙氨酸向(R)-β-芳基丙氨酸的转化得到增强
    标题:通过消旋酶/氨基酸突变酶催化,外消旋α-芳基丙氨酸向(R)-β-芳基丙氨酸的转化得到增强
    摘要:的红豆杉苯基丙氨酸氨基变位酶(pam)酶转换数(小号)-α-Arylalanines到其相应的(-[r)-β-Arylalanines.将各种外消旋底物与100μgpam在31oc下孵育20小时后,将每个(S)-α-芳基丙氨酸对映异构体异构化为其相应的(R)-β-产物.对于外消旋原料,(R)-β-芳基丙氨酸产物与(S)-α-底物的比例在0.4至1.8之间,并且剩余的非生产性(R)-α-芳基丙氨酸变得富集.为了利用(R)-α-异构体,恶臭假单胞菌的混杂丙氨酸消旋酶的催化作用(kt2440)与pam偶联可增加外消旋α-芳基丙氨酸底物对映体纯(R)-β-芳基丙氨酸的产量.包括生物催化消旋作用和pam催化反应在内,对映纯β-芳基丙氨酸的总反应产率在4%至19%之间(取决于芳基丙氨酸)适度提高了,与之相比,增加了63%.仅用氨基变位酶反应即可实现更替.串联使用这些生物催化剂可能会在手性β-芳基丙氨
    Doi:10.1021/jo9009563

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    专利信息


    专利号:US-4891442-A
    优先权日:1987-03-09
    标 题 :Process for synthesis of β-phenylalanine
    发明人:LIN JIANG-JEN; KNIFTON JOHN F
    权利人:TEXACO INC
    摘要:N-acetyl-β-phenylalanine is synthesized by reacting phenylacetaldehyde, acetamide and synthesis gas with a catalyst comprising a cobalt-containing compound in conjunction with a cocatalyst that may be either a Group VB or VIB containing ligand, or a rhodium compound optionally bonded to one or more Group VB or VIB donor ligands, at a temperature of at least 50° C. and a pressure of at least 500 psi.

    专利号:US-2023037284-A9
    优先权日:2018-11-30
    标题:Combination therapy of peptidomimetic macrocycles
    发明人:GUERLAVAIS VINCENT; ANNIS DAVID ALLEN
    权利人:AILERON THERAPEUTICS INC
    摘要:The present disclosure describes the synthesis of peptidomimetic macrocycles and methods of using peptidomimetic macrocycles to treat a condition. The present disclosure also describes methods of using peptidomimetic macrocycles in combination with at least one additional pharmaceutically-active agent for the treatment of a condition, for example, cancer.

    专利号:US-9453037-B2
    优先权日:2011-07-28
    标 题 :Methylphenidate-prodrugs, processes of making and using the same
    发明人:GUENTHER SVEN; CHI GUOCHEN; BERA BINDU; MICKLE TRAVIS; BERA SANJIB
    权利人:KEMPHARM INC; KEMPHARM INC
    摘要:The present technology is directed to prodrugs and compositions for the treatment of various diseases and/or disorders comprising methylphenidate, or methylphenidate derivatives, conjugated to at least one alcohol, amine, oxoacid, thiol, or derivatives thereof. In some embodiments, the conjugates further include at least one linker. The present technology also relates to the synthesis of methylphenidate, or methylphenidate derivatives, conjugated to at least one alcohol, amine, oxoacid, thiol, or derivatives thereof or combinations thereof.

    专利号:US-9574189-B2
    优先权日:2005-12-01
    标题:Enzymatic encoding methods for efficient synthesis of large libraries
    发明人:FRANCH THOMAS; LUNDORF MIKKEL DYBRO; JACOBSEN SØREN NYBOE; OLSEN EVA KAMPMANN; ANDERSEN ANNE LEE; HOLTMANN ANETTE; HANSEN ANDERS HOLM; SØRENSEN ANDERS MALLING; GOLDBECH ANNE; DE LEON DAEN; KALDOR DITTE KIEVSMOSE; SLØK FRANK ABILDGAARD; HUSEMOEN GITTE NYSTRUP; DOLBERG JOHANNES; Jensen Kim Birkebæ; PEDERSEN LENE; NØRREGAARD-MADSEN MADS; GODSKESEN MICHAEL ANDERS; GLAD SANNE SCHRØDER; NEVE SØREN; THISTED THOMAS; KRONBORG TINE TITILOLA AKINLEMINU; SAMS CHRISTIAN KLARNER; FELDING JAKOB; FRESKGÃ…RD PER-OLA; GOULIAEV ALEX HAAHR; PEDERSEN HENRIK
    权利人:FRANCH THOMAS; LUNDORF MIKKEL DYBRO; JACOBSEN SØREN NYBOE; OLSEN EVA KAMPMANN; ANDERSEN ANNE LEE; HOLTMANN ANETTE; HANSEN ANDERS HOLM; SØRENSEN ANDERS MALLING; GOLDBECH ANNE; DE LEON DAEN; KALDOR DITTE KIEVSMOSE; SLØK FRANK ABILDGAARD; HUSEMOEN GITTE NYSTRUP; DOLBERG JOHANNES; Jensen Kim Birkebæ; PEDERSEN LENE; NØRREGAARD-MADSEN MADS; GODSKESEN MICHAEL ANDERS; GLAD SANNE SCHRØDER; NEVE SØREN; THISTED THOMAS; KRONBORG TINE TITILOLA AKINLEMINU; SAMS CHRISTIAN KLARNER; FELDING JAKOB; FRESKGÃ…RD PER-OLA; GOULIAEV ALEX HAAHR; PEDERSEN HENRIK; NUEVOLUTION AS
    摘要:Disclosed is a method for obtaining a bifunctional complex comprising a molecule linked to a single stranded identifier oligonucleotide, wherein a nascent bifunctional complex comprising a chemical reaction site and a priming site for enzymatic addition of a tag is a) reacted at the chemical reaction site with one or more reactants, and b) reacted enzymatically at the priming site with one or more tag(s) identifying the reactant(s).

    专利号:US-2025084410-A1
    优先权日:2015-01-12
    标 题:Incorporation of unnatural nucleotides and methods thereof
    发明人:PTACIN JEROD; MALYSHEV DENIS A; CAFFARO CAROLINA E
    权利人:SYNTHORX INC
    摘要:Disclosed herein are methods, compositions and kits for the synthesis of proteins which comprises unnatural amino acids that utilize a mutant tRNA.

    专利号:US-2018371021-A1
    优先权日:2017-05-11
    标 题 :Peptidomimetic macrocycles and uses thereof
    发明人:AIVADO MANUEL; GUERLAVAIS VINCENT; OLSON KAREN
    权利人:AILERON THERAPEUTICS INC
    摘要:The present disclosure describes the synthesis of peptidomimetic macrocycles and methods of using peptidomimetic macrocycles to treat a condition. The present disclosure also describes methods of using peptidomimetic macrocycles in combination with at least one additional pharmaceutically-active agent for the treatment of a condition, for example, cancer.
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    合成参考文献


    摘要:Nguyen, B. N.; Hii, K. K.; Szymański, W.; Janssen, D. B., Science of Synthesis: Stereoselective Synthesis, (2011) 1, 643.
    摘要:Faber, K.; Glueck, S. M., Science of Synthesis: Biocatalysis in Organic Synthesis, (2015) 1, 476.
    摘要:Bartsch, S.; Vogel, A., Science of Synthesis: Biocatalysis in Organic Synthesis, (2015) 2, 306.
    摘要:Slomka, C.; Engel, U.; Syldatk, C.; Rudat, J., Science of Synthesis: Biocatalysis in Organic Synthesis, (2015) 1, 403.
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