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    • 22. 发明申请
    • Novel carbonyl reductase, gene thereof and use of the same
    • 新型羰基还原酶,其基因及其用途
    • US20060046289A1
    • 2006-03-02
    • US10512908
    • 2003-04-30
    • Noriyuki KizakiMiho HorikawaYoshihiko Yasohara
    • Noriyuki KizakiMiho HorikawaYoshihiko Yasohara
    • C12P7/22C07H21/04C12P21/06C12N9/02C12N1/21
    • C12N9/0006C12Y101/01184
    • The present invention provides a novel polypeptide forming (R)-2-chloro-1-(3′-chlorophenyl)ethanol, a polynucleotide coding for said polypeptide, and use of the same. The present invention relates to a polypeptide having the following physical and chemical properties (1) to (4): (1) activity: acting on 2-chloro-1-(3′-chlorophenyl)ethanone with NADPH or NADH as a coenzyme, to form (R)-2-chloro-1-(31-chlorophenyl)ethanol; (2) optimum pH for activity: 5.0 to 6.0; (3) optimum temperature for activity: 40° C. to 50° C.; (4) molecular weight: about 40,000 as determined by gel filtration analysis, about 30,000 as determined by SDS polyacrylamide gel electrophoresis analysis. The present invention also relates to a polypeptide comprising the amino acid sequence shown under SEQ ID NO:1 in the sequence listing, a polynucleotide coding for said polypeptide, and a transformant producing said polypeptide at high levels.
    • 本发明提供形成(R)-2-氯-1-(3'-氯苯基)乙醇的新型多肽,编码所述多肽的多核苷酸及其用途。 本发明涉及具有以下物理和化学性质(1)至(4)的多肽:(1)活性:以NADPH或NADH作为辅酶作用于2-氯-1-(3'-氯苯基)乙酮, 形成(R)-2-氯-1-(31-氯苯基)乙醇; (2)活性最佳pH:5.0〜6.0; (3)最适温度为40℃〜50℃。 (4)分子量:约40,000,通过凝胶过滤分析测定,约30,000,通过SDS聚丙烯酰胺凝胶电泳分析测定。 本发明还涉及包含序列表中SEQ ID NO:1所示氨基酸序列的多肽,编码所述多肽的多核苷酸,以及以高水平产生所述多肽的转化体。
    • 23. 发明申请
    • Process for preparing optically active 2-[6-(hydroxy-methyl)-1,3-dioxan-4-yl] acetic acid derivatives
    • 光学活性的2- [6-(羟基 - 甲基)-1,3-二恶烷-4-基]乙酸衍生物的制备方法
    • US20050080277A1
    • 2005-04-14
    • US10048553
    • 2001-06-05
    • Akira NishiyamaMiho HorikawaYoshihiko YasoharaNoboru UeyamaKenji Inoue
    • Akira NishiyamaMiho HorikawaYoshihiko YasoharaNoboru UeyamaKenji Inoue
    • C07D319/06C12P7/42C12P17/06
    • C07D319/06C12P7/42C12P17/06
    • The present invention is to provide a production technology by which an optically active 2-[6-(hydroxymethyl)-1,3-dioxan-4-yl]acetic acid derivative, which are of value as pharmaceutical intermediates, can be produced from inexpensive and readily available starting materials without using any extraordinary equipment such as an ultra-low-temperature reactor. The present invention is a production process of an optically active 2-[6-(hydroxymethyl)-1,3-dioxan-4-yl]acetic acid derivative which comprises reacting an enolate, prepared by permitting a base or a 0-valent metal to act on an acetic acid ester derivative with (S)-β-hydroxy-γ-butyrolactone at a temperature not lower than −30° C. to give a dihydroxyoxohexanoic acid derivative, treating the same with an acylating agent in the presence of a base to produce a dihydroxyoxohexanoic acid monoacyl derivative, reducing this compound with a microorganism to produce a trihydroxyhexanoic acid monoacyl derivative, treating this compound with an acetal-forming reagent in the presence of an acid catalyst to produce an acyloxymethyldioxanylacetic acid derivative, and finally, subjecting this compound to solvolysis in the presence of a base.
    • 本发明提供一种生产技术,通过该技术,可以以廉价的方式生产价值为医药中间体的光学活性的2- [6-(羟甲基)-1,3-二恶烷-4-基]乙酸衍生物 和容易获得的起始材料,而不使用任何非常设备,例如超低温反应器。 本发明是光学活性的2- [6-(羟甲基)-1,3-二恶烷-4-基]乙酸衍生物的制备方法,该方法包括使通过使碱或0价金属 在不低于-30℃的温度下用(S)-β-羟基-γ-丁内酯在乙酸酯衍生物上作用,得到二羟基氧代己酸衍生物,在酰化剂存在下用酰化剂处理 碱化以制备二羟基氧己基单酰基衍生物,用微生物还原该化合物以产生三羟基己酸单酰基衍生物,在酸催化剂存在下用缩醛形成试剂处理该化合物,得到酰氧基甲基二恶烷基乙酸衍生物,最后, 该化合物在碱存在下溶剂解。