METHOD FOR CRYSTALLIZATION OF 2-AMINO-2-Ý2-Ý4-(3- BENZYLOXYPHENYLTHIO)-2-CHLOROPHENYL¨ETHYL¨-1,3-PROPANEDIOL HYDROCHLORIDE
    9.
    发明公开
    METHOD FOR CRYSTALLIZATION OF 2-AMINO-2-Ý2-Ý4-(3- BENZYLOXYPHENYLTHIO)-2-CHLOROPHENYL¨ETHYL¨-1,3-PROPANEDIOL HYDROCHLORIDE 有权
    VERFAHREN ZUR KRISTALLISIERUNG VON 2-AMINO-2-| 2-| 4-(3-苄氧基苯基)-2-氯苯基乙基-1,3-丙二醇氯仿

    公开(公告)号:EP2269982A4

    公开(公告)日:2014-03-12

    申请号:EP09724232

    申请日:2009-03-18

    申请人: KYORIN SEIYAKU KK

    IPC分类号: C07C319/28 C07C323/32

    摘要: The present invention herein provides a method for highly efficiently preparing high purity crystals of 2-amino-2-[2-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]-ethyl]-1,3-propanediol hydrochloride. The method comprises the following steps: (1) dissolving 2-amino-2-[2-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]ethyl]-1,3-propanediol in a mixed solvent comprising a solvent in which the compound in the form of the hydrochloride thereof is highly soluble and a solvent in which the compound in its hydrochloride is less soluble, to thus prepare a solution of 2-amino-2-[2-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]ethyl]-1,3-propanediol; and then (2) adding hydrochloric acid to the resultant solution with stirring, to thus crystallize the hydrochloride of 2-amino-2-[2-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]ethyl]-1,3-propanediol.

    摘要翻译: 本发明提供了高效制备2-氨基-2- [2- [4-(3-苄氧基苯硫基)-2-氯苯基] - 乙基] -1,3-丙二醇盐酸盐的高纯度晶体的方法。 该方法包括以下步骤:(1)将2-氨基-2- [2-(4-(3-苄氧基苯硫基)-2-氯苯基]乙基] -1,3-丙二醇溶于包含其中的溶剂的混合溶剂中, 其盐酸盐形式的化合物是高度可溶的,其中其盐酸盐中的化合物较不溶解的溶剂,从而制备2-氨基-2- [2- [4-(3-苄氧基苯硫基) - 2-氯苯基]乙基] -1,3-丙二醇; 然后(2)在搅拌下向所得溶液中加入盐酸,从而使2-氨基-2- [2- [4-(3-苄氧基苯硫基)-2-氯苯基]乙基] -1,3- 丙二醇。

    METHOD FOR PRODUCING 3,4-DISUBSTITUTED PYRROLIDINE DERIVATIVE
    10.
    发明公开
    METHOD FOR PRODUCING 3,4-DISUBSTITUTED PYRROLIDINE DERIVATIVE 审中-公开
    用于生产3,4-二取代吡咯烷

    公开(公告)号:EP2634172A4

    公开(公告)日:2014-01-29

    申请号:EP11836226

    申请日:2011-10-24

    申请人: KYORIN SEIYAKU KK

    摘要: The present invention provides an inexpensive and industrially advantageous method for producing an optically active form of an anti-(3S,4R)-3-alkylcarbamoyl-4-hydroxypyrrolidine derivative or it's enantiomer, which is a key intermediate for producing a high-quality optically active form of (3R,4S)-3-alkylaminomethyl-4-fluoropyrrolidine or it's enantiomer useful as an intermediate for producing pharmaceuticals. The present invention relates to a method for producing an optically active anti-(3S,4R)-4-hydroxypyrrolidine-3-carboxamide derivative, or it's enantiomer by carrying out asymmetric hydrogenation using an optically active catalyst of a 4-oxopyrrolidine-3-carboxamide derivative represented by the general formula (I). [in the formula (I), PG 1 represents a protective group for an amino group, and R 1 represents hydrogen, a C1 to C6 alkyl group which may be substituted, or a C3 to C8 cycloalkyl group which may be substituted].