CAS: 32133-36-1; 3,4-Difluorophenylalanine

该化合物是苯丙烯的氟化衍生物,其特点是在苯环的3和4个位置用氟代替氢原子,这一修改增强了其在药用化学和浸泡物研究中的效用,在这种研究中,氟的结合可以提高代谢稳定性,生物利用率和结合性.该化合物是设计酶抑制剂,受体离子体和生物活性浸泡物的宝贵建筑材料.其结构特征使得它特别有助于研究结构-活性关系(SAR)和优化药用动力学特性.氟原子的存在也有助于在PET成像和放射标签研究中的应用.高纯度和持续质量确保合成应用的可靠性能.

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198474-90-7 198560-43-9 205445-51-8

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CAS号2927-34-6 3,4-二氟甲苯 | CAS号85118-01-0 3,4-二氟溴苄

合成工艺路线路线简述

    3,4-二氟甲苯置于盐酸,N-溴代丁二酰亚胺(Nbs),溶剂黄146,过氧化苯甲酰体系中,化学反应生成3,4-二氟-Dl-苯丙氨酸
    参考文献:实验诱导的苯丙酮尿症.I.苯丙氨酸羟化酶的抑制剂.
    标题:实验诱导的苯丙酮尿症.I.苯丙氨酸羟化酶的抑制剂.
    摘要:
    Doi:10.1021/jm00313A013

    海关参考信息

    专利信息


    专利号:US-9938509-B2
    优先权日:2010-12-08
    标 题 :Biocatalysts and methods for the synthesis of armodafinil
    发明人:ANG EE LUI; ALVIZO OSCAR; BEHROUZIAN BEHNAZ; CLAY MICHAEL D; COLLIER STEVEN J; EBERHARD ELLEN D; FAN FU; SONG SHIWEI; SMITH DEREK J; WIDEGREN MAGNUS; WILSON ROBERT; XU JUNYE; ZHU JUN
    权利人:CODEXIS INC
    摘要:The present invention relates to non-naturally occurring polypeptides useful for preparing armodafinil, polynucleotides encoding the polypeptides, and methods of using the polypeptides. The non-naturally occurring polypeptides of the present invention are effective in carrying out biocatalytic conversion of the (i) 2-(benzhydrylsulfinyl)acetamide to (−)-2-[(R)-(diphenylmethyl)sulfinyl]acetamide (armodafinil), or (ii) benzhydryl-thioacetic acid to (R)-2-(benzhydrylsulfinyl)acetic acid, which is a pivotal intermediate in the synthesis of armodafinil, in enantiomeric excess.

    专利号:US-9206222-B2
    优先权日:2009-06-29
    标题:Solid phase peptide synthesis of peptide alcohols
    发明人:CAUSSIL-AMBLARD MURIEL; MARTINEZ JEAN; TAILHADES JULIEN
    权利人:CAUSSIL-AMBLARD MURIEL; MARTINEZ JEAN; TAILHADES JULIEN; CENTRE NAT RECH SCIENT
    摘要:The present invention relates to the synthesis of depsipeptides on solid phase support. Said depsipeptides are then implicated in a solution phase O—N acyl shift enabling to obtain the corresponding peptide alcohols.

    专利号:US-9663771-B2
    优先权日:2013-01-18
    标题 :Engineered biocatalysts useful for carbapenem synthesis
    发明人:SUKUMARAN JOLY; SMITH DEREK; YANG HONG; YEO WAN LIN; MOORE JEFFREY C
    权利人:CODEXIS INC
    摘要:The present disclosure provides engineered pNB esterase polypeptides useful for the synthesis of the carbapenem antibiotic, imipenem. The disclosure also provides polynucleotides encoding the engineered pNB esterases, host cells capable of expressing the engineered pNB esterases, and methods of using the engineered pNB esterases in the production of imipenem.

    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-12410410-B2
    优先权日:2015-02-10
    标题 :Ketoreductase polypeptides for the synthesis of chiral compounds
    发明人:ALVIZO OSCAR; AGARD NICHOLAS J; XIE XINKAI; ENTWISTLE DAVID; KOSJEK BIRGIT
    权利人:CODEXIS INC
    摘要:The present disclosure provides engineered ketoreductase enzymes having improved properties as compared to a naturally occurring wild-type ketoreductase enzyme. Also provided are polynucleotides encoding the engineered ketoreductase enzymes, host cells capable of expressing the engineered ketoreductase enzymes, and methods of using the engineered ketoreductase enzymes to synthesize a variety of chiral compounds.

    专利号:US-8932838-B2
    优先权日:2010-06-17
    标 题 :Biocatalysts and methods for the synthesis of (S)-3-(1-aminoethyl)-phenol
    发明人:CABIROL FABIEN LOUIS; GOHEL ANUPAM; OH SEONG HO; SMITH DEREK J; WONG BRIAN; LALONDE JAMES J
    权利人:CODEXIS INC
    摘要:The present disclosure provides engineered transaminase polypeptides having improved properties as compared to naturally occurring transaminases including the ability of converting the substrate, 3′-hydroxyacetophenone to (S)-3-(1-aminoethyl)-phenol in enantiomeric excess and high percentage conversion. Also provided are polynucleotides encoding the engineered transaminases, host cells capable of expressing the engineered transaminases, and methods of using the engineered transaminases to synthesize (S)-3-(1-aminoethyl)-phenol and related compounds useful in the production of active pharmaceutical ingredients.
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    主要参考文献

    [参考文献]: Piepenbrink Kh, Et Al. Fluorine Substitutions In An Antigenic Peptide Selectively Modulate T-Cell Receptor Binding In A Minimally Perturbing Manner. Biochem J. 2009 Oct 12;423(3):353-61.
    [参考文献]: Ravarino P, Et Al. Fluorine Effect In The Gelation Ability Of Low Molecular Weight Gelators. Gels. 2022 Feb 8;8(2):98.
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