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    Process for the preparation of optically pure 4-hydroxy-2-oxo-1-pyrrolidine acetamide
    5.
    发明申请
    Process for the preparation of optically pure 4-hydroxy-2-oxo-1-pyrrolidine acetamide 审中-公开
    制备光学纯的4-羟基-2-氧代-1-吡咯烷乙酰胺的方法

    公开(公告)号：US20070185337A1

    公开(公告)日：2007-08-09

    申请号：US11596580

    申请日：2005-05-25

    申请人： Seong-Jin Kim ,  Chung-woo Lim ,  Chang Boo ,  Jung-hoon Oh ,  Ki Kim ,  Jae Lee ,  Duk Won

    发明人： Seong-Jin Kim ,  Chung-woo Lim ,  Chang Boo ,  Jung-hoon Oh ,  Ki Kim ,  Jae Lee ,  Duk Won

    IPC分类号： C07D207/04

    CPC分类号： C07D207/273

    摘要： A process for the preparation of chiral 4-hydroxy-2-oxo-1-pyrrolidine acetamide includes adding sodium cyanide together with citric acid to a solution of chiral epichlorohydrin to obtain chiral 3-chloro-2-hydroxypropionitrile by ring opening reaction of the chiral epichlorohydrin, reacting the obtained product with an alcohol containing hydrochloride gas to obtain chiral 4-chloro-3-hydroxybutyric acid ester, and reacting the obtained product in a presence of a base with glycinamide or with glycine ester accompanied by ammonolysis with ammonia to produce the targeted chiral 4-hydroxy-2-oxo-1-pyrrolidine acetamide.

    摘要翻译： 手性4-羟基-2-氧代-1-吡咯烷乙酰胺的制备方法包括将氰化钠与柠檬酸一起加入到手性表氯醇的溶液中，以通过手性的开环反应获得手性3-氯-2-羟基丙腈 将得到的产物与含有盐酸气体的醇反应，得到手性4-氯-3-羟基丁酸酯，并使得到的产物在碱的存在下与甘氨酰胺或甘氨酸酯反应，伴随着氨的氨解，生成 靶向手性4-羟基-2-氧代-1-吡咯烷乙酰胺。

    Process for the preparation of highly optical pure carvedilol
    9.
    发明授权
    Process for the preparation of highly optical pure carvedilol 有权
    制备高光学纯卡维地洛的方法

    公开(公告)号：US08101781B2

    公开(公告)日：2012-01-24

    申请号：US12280684

    申请日：2006-08-31

    申请人： Seong-Jin Kim ,  Chang Woo Jong ,  Hyun Bin Kang ,  Byung Hyun Moon ,  Long Guo Quan ,  Duk Kwon Won ,  Kyung Yong Jin

    发明人： Seong-Jin Kim ,  Chang Woo Jong ,  Hyun Bin Kang ,  Byung Hyun Moon ,  Long Guo Quan ,  Duk Kwon Won ,  Kyung Yong Jin

    IPC分类号： A61K31/403 ,  C07D209/88

    CPC分类号： C07D209/88 ,  C07D263/24 ,  C07D413/12 ,  Y02P20/55

    摘要： The present invention relates to a process for the efficient preparation of highly optical pure chiral carvedilol. According to the present invention, a chiral oxazolidin-2-one or oxazolidin-2-thione having formula 2, produced from the reaction of N-protected 2-(2-methoxyphenoxy)ethylamine with a chiral glycidol derivative is used as a key intermediate for the preparation of the chiral carvedilol. Specifically, the process for the preparation of the chiral carvedilol comprises a) reacting a compound of formula 2 with a halogenation agent, a sulfonation agent or a mitsunobu reagent to activate a hydroxyl group of the compound of formula 2, followed by nucleophilic substitution reaction with 9H-4-hydroxy carbazole to produce a compound of formula 7, and b) subjecting the obtained compound of formula 7 to a deprotection reaction in a presence of an inorganic base to produce the targeted chiral carvedilol. The process of the present invention can be accomplished in a mild condition. The process neither requires any extraordinary purification procedure, nor involves decrease of optical purity. Therefore, the process of the present invention provides highly optical pure chiral carvedilol in simple and efficient manner.

    摘要翻译： 本发明涉及高效光学纯手性卡维地洛的高效制备方法。 根据本发明，由N-保护的2-（2-甲氧基苯氧基）乙胺与手性缩水甘醇衍生物的反应生成的具有式2的手性恶唑烷-2-酮或恶唑烷-2-硫酮用作关键中间体 用于制备手性卡维地洛。 具体地说，制备手性卡维西洛的方法包括：a）使式2的化合物与卤化剂，磺化剂或mitsunobu试剂反应以活化式2化合物的羟基，然后与 9H-4-羟基咔唑制备式7的化合物，和b）在无机碱的存在下使得到的式7的化合物进行脱保护反应，得到目标的手性卡维地洛。 本发明的方法可以在温和的条件下完成。 该方法既不需要任何非凡的纯化程序，也不涉及降低光学纯度。 因此，本发明的方法以简单有效的方式提供高光学纯手性卡维地洛。