CAS: 114926-38-4; 4-(Trifluoromethyl)-L-Phenylalanine

该化合物是一种非天然的氨基酸衍生物,在苯环的副位置上有一个三氟甲基组,这种改变增强了其消毒和电子特性,使其在药用化学和peptide研究中具有宝贵价值;三氟甲基组改善了代谢稳定性和亲脂性,促进了生物活性化合物中的膜渗透性;其气力L配置确保了与天然peptide合成协议的兼容性;该化合物在酶抑制剂,受体离子和生物活性的氟化类似物的设计中特别有用;其结构多功能使得分子相互作用得到精确的调整,使其成为药物发现和生物化学研究中的一个关键建筑块.

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114872-99-0 114873-07-3 238742-88-6

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(S)-2-amino-3-(4-(trifluoromethyl)phenyl)propanoic acid methyl ester 4-Trifluoromethylbenzaldehyde (Z)-2-methyl-4-[4-(trifluoromethyl)benzylidene]-5(4H)-oxazolone 4-bromomethyltrifluoromethylbenzene N-tert-butoxycarbonyl-L-4-trifluoromethylphenylalanine tert-butyl (S)-(1-(benzyl(methyl)amino)-1-oxo-3-(4-(trifluoromethyl)phenyl)propan-2-yl)carbamate (2S,4R)-2-[(S)-1-(Benzyl-methyl-carbamoyl)-2-(4-trifluoromethyl-phenyl)-ethylcarbamoyl]-4-hydroxy-pyrrolidine-1-carboxylic acid tert-butyl ester (S)-2-[(S)-2-(2-{2-[(S)-2-Amino-3-(4-hydroxy-phenyl)-propionylamino]-acetylamino}-acetylamino)-3-(4-trifluoromethyl-phenyl)-propionylamino]-4-methyl-pentanoic acid; hydr°Chloride

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    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-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-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-2022243244-A1
    优先权日:2019-10-10
    标 题 :Compositions and methods for in vivo synthesis of unnatural polypeptides
    发明人:ROMESBERG FLOYD E; FISCHER EMIL C; HASHIMOTO KOJI; FELDMAN AARON W; DIEN VIVIAN T; ZHANG YORKE
    权利人:SCRIPPS RESEARCH INST
    摘要:Disclosed herein are compositions, methods, and kits for a cell incorporating unnatural amino acids into an unnatural polypeptide. Also disclosed herein are compositions, methods, and kits for increasing activity and yield of the unnatural polypeptide synthesized by the cell.

    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.
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    主要参考文献

    [参考文献]: Luckose F, Et Al. Effects Of Amino Acid Derivatives On Physical, Mental, And Physiological Activities. Crit Rev Food Sci Nutr. 2015;55(13):1793-807.

    合成参考文献


    摘要:Parmeggiani, F.; Galman, J. L.; Montgomery, S. L.; Turner, N. J., Science of Synthesis, (2019) , 408.
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