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    • 6. 发明授权
    • Production of chirally pure &agr;-amino acids and N-sulfonyl &agr;-amino acids
    • 手性纯α-氨基酸和N-磺酰基α-氨基酸的生产
    • US06657070B2
    • 2003-12-02
    • US10166896
    • 2002-06-11
    • Lynn Resnick
    • Lynn Resnick
    • C07D33332
    • C07D307/64C07D333/34C07D409/12
    • Methods for production of chirally pure &agr;-amino acids and N-sulfonyl &agr;-amino acids are described. An aldehyde and a cyanide salt are reacted with an &agr;-methylbenzylamine to afford product. The product reacts with a strong acid, neutralized, and extracted. The resulting product is hydrolyzed to provide a product which is dissolved in a strong acid to provide a salt of a chirally pure &agr;-amino acid, which is reacted to provide the chirally pure &agr;-amino acid. Another method involves mixing ephedrine hemihydrate and an N-sulfonyl &agr;-ethylnorvaline in ethanol at a molar ratio of 1:1; heating the mixture to dissolve the solids; cooling to allow formation of a precipitate; washing with an organic solvent to give diastereomeric salt; recrystallizing the salt; dissolving the recrystallized salt in an organic solvent and strong aqueous acid, separating the layers; washing the organic extract; drying and concentrating to provide chirally pure N-sulfonyl &agr;-amino acid.
    • 描述了生产手性纯α-氨基酸和N-磺酰基α-氨基酸的方法。 使醛和氰化物盐与α-甲基苄胺反应得到产物。 产物与强酸反应,中和并萃取。 将所得产物水解以提供溶解在强酸中以产生手性纯的α-氨基酸的盐的产物,其被反应以提供手性纯的α-氨基酸。 另一种方法包括以摩尔比1:1混合乙醇中的麻黄碱半水合物和N-磺酰基α-乙基缬氨酸; 加热混合物以溶解固体; 冷却以形成沉淀物; 用有机溶剂洗涤得到非对映体盐; 重结晶盐; 将重结晶盐溶解在有机溶剂和强酸性水溶液中,分离各层; 洗涤有机提取物; 干燥和浓缩以提供手性纯的N-磺酰基α-氨基酸。
    • 10. 发明授权
    • Process for the synthesis of chirally pure beta-amino-alcohols
    • 手性纯合β-氨基醇的合成方法
    • US06800764B2
    • 2004-10-05
    • US10304322
    • 2002-11-26
    • Anthony Frank KreftMadelene Miyoko AntaneDerek Cecil ColeDennis Martin KubrakLynn ResnickJoseph Raymond StockZheng Wang
    • Anthony Frank KreftMadelene Miyoko AntaneDerek Cecil ColeDennis Martin KubrakLynn ResnickJoseph Raymond StockZheng Wang
    • C07D33332
    • C07C215/20C07B2200/07C07C215/08C07C215/24C07C215/28C07C215/56C07C229/08C07C229/28C07C229/30C07C229/36C07C247/12C07C323/63C07D263/26C07D333/34
    • A process is provided for preparing chirally pure S-enantiomers of &agr;-amino acids comprising the steps of: a) preparing an organometallic reagent from an alkyl halide of the formula (R)2CH(CH2)nCH2X; b) adding the organometallic reagent to carbon dioxide to afford a carboxylic acid; c) activating the carboxylic acid with an acid chloride, phosphorus trichloride, acid anhydride, or thionyl chloride in the presence of a tertiary amine base; d) reacting the product of step c) with an alkali metal salt of S-4-benzyl-2-oxazolidinone; e) treating the product of step d) with a strong non-nucleophilic base to form an enolate anion; f) trapping the enolate anion with 2,4,6-triisopropylbenzenesulfonyl azide to afford an oxazolidinone azide; g) hydrolyzing the oxazolidinone azide with an aqueous base to afford an &agr;-azido acid; h) reducing the &agr;-azido acid to the &agr;-amino acid; and i) recrystallizing the &agr;-amino acid to the chirally pure &agr;-amino acid. A process is also provided for preparing chirally pure S-enantiomers of &bgr;-amino alcohols further comprising the steps of reducing the crude &agr;-amino acid to the &bgr;-amino alcohol and recrystallizing the &bgr;-amino alcohol to the chirally pure &bgr;-amino alcohol. A process is further provided for preparing chirally pure S enantiomers of N-sulfonyl &bgr;-amino alcohols further comprising the steps of sulfonylating the &bgr;-amino alcohol with 5-chloro-thiophene-2-sulfonyl halide; and recrystallizing to afford the chirally pure N-sulfonyl &bgr;-amino alcohols.
    • 提供了一种用于制备α-氨基酸的手性纯的S-对映异构体的方法,包括以下步骤:a)由式(R)2CH(CH 2)n CH 2 X的烷基卤制备有机金属试剂; b)将有机金属试剂加入到二氧化碳中,得到羧酸; c)在叔胺碱存在下用酰氯,三氯化磷,酸酐或亚硫酰氯活化羧酸; d)使步骤c)的产物与S-4-苄基-2-恶唑烷酮的碱金属盐反应; e)用强非亲核碱处理步骤d)的产物以形成烯醇化物阴离子; f)用2,4,6-三异丙基苯磺酰叠氮化物捕获烯醇化阴离子,得到恶唑烷酮叠氮化物; g)用碱水溶液水解恶唑烷酮叠氮化物,得​​到α-叠氮基; h)将α-叠氮基还原成α-氨基酸; 和i)将α-氨基酸重结晶至手性纯的α-氨基酸。 还提供了制备β-氨基醇的手性纯的S-对映异构体的方法,该方法还包括将β-氨基酸的粗α-氨基酸还原成β-氨基醇,并将β-氨基醇重结晶至手性纯的β-氨基醇 。 还提供了制备N-磺酰基β-氨基醇的手性纯S对映异构体的方法,其还包括用5-氯 - 噻吩-2-磺酰卤磺酰化β-氨基醇的步骤; 并重结晶得到手性纯的N-磺酰基β-氨基醇。