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    Process for the preparation of substituted thiazolines and their intermediates
    2.
    发明授权
    Process for the preparation of substituted thiazolines and their intermediates 失效
    制备取代噻唑啉及其中间体的方法

    公开(公告)号：US06894170B2

    公开(公告)日：2005-05-17

    申请号：US10270324

    申请日：2002-10-15

    申请人： Sylvia Krich ,  Alexander Rieder ,  Ferdinand Heu ,  Gerhard Steinbauer

    发明人： Sylvia Krich ,  Alexander Rieder ,  Ferdinand Heu ,  Gerhard Steinbauer

    IPC分类号： C12P41/00 ,  C07B55/00 ,  C07B57/00 ,  C07C319/02 ,  C07C319/28 ,  C07C323/58 ,  C07D277/12 ,  C07D417/04 ,  C07D277/10

    CPC分类号： C07D417/04 ,  C07C319/02 ,  C07D277/12 ,  C07C323/58

    摘要： Process for the preparation of substituted thiazolines of the formula (I) in which Ar is a phenyl, naphthyl, thienyl, pyridyl or quinolinyl radical which can optionally be substituted by one or more substituents from the group consisting of halogen, OH, benzyloxy, C1-C4-alkyl, C1-C4-alkoxy, COOR1 where R1 is H or C1-C4-alkyl, by coupling of (S)-α-methylcysteine hydrochloride of the formula (II) with a nitrile of the formula (III) Ar—CN in which Ar is as defined above, or a corresponding C1-C4-alkyl imidate, in which (S)-α-methylcysteine hydrochloride of the formula (II) is reacted in a suitable solvent with a nitrile of the formula (III) or a corresponding C1-C4-alkyl imidate in the presence of a tertiary base at a pH of 6.5 to 10 at 50° C. up to the reflux temperature to give the corresponding thiazoline of the formula (I), and processes for the preparation of (S)-α-methylcysteine hydrochloride and its use for the preparation of thiazolines of the formula (I).

    摘要翻译： 制备式（I）的取代噻唑啉的方法，其中Ar是苯基，萘基，噻吩基，吡啶基或喹啉基，其可以任选地被一个或多个选自卤素，OH，苄氧基，C C 1 -C 4 - 亚烷基，C 1 -C 4 - 烷氧基，COOR 1 - 其中R 1是H或C 1 -C 4 - 烷基，通过将（S）-α-甲基半胱氨酸盐酸盐与 式（II）与式（III）的腈<？in-line-formula description =“In-line formula”end =“lead”？> Ar-CN <？in-line-formula description =“In- 其中Ar如上所定义，或其相应的C 1 -C 4 - 亚烷基亚氨酸酯，其中（S） - 式（II）的α-甲基半胱氨酸盐酸盐在合适的溶剂中与式（III）的腈或相应的C 1 -C 4 - 亚烷基亚氨基酯反应 在pH为6.5t的叔碱存在下进行 o 10在50℃直到回流温度，得到相应的式（I）噻唑啉，以及制备（S）-α-甲基半胱氨酸盐酸盐的方法及其用于制备式（I）的噻唑啉的用途 一世）。

    Process for the preparation of substituted thiazolines and their intermediates
    3.
    发明申请
    Process for the preparation of substituted thiazolines and their intermediates 审中-公开
    制备取代噻唑啉及其中间体的方法

    公开(公告)号：US20050101782A1

    公开(公告)日：2005-05-12

    申请号：US11011110

    申请日：2004-12-15

    申请人： Sylvia Krich ,  Alexander Rieder ,  Ferdinand Heu ,  Gerhard Steinbauer

    发明人： Sylvia Krich ,  Alexander Rieder ,  Ferdinand Heu ,  Gerhard Steinbauer

    IPC分类号： C12P41/00 ,  C07B55/00 ,  C07B57/00 ,  C07C319/02 ,  C07C319/28 ,  C07C323/58 ,  C07D277/12 ,  C07D417/04

    CPC分类号： C07D417/04 ,  C07C319/02 ,  C07D277/12 ,  C07C323/58

    摘要： Process for the preparation of substituted thiazolines of the formula (I) in which Ar is a phenyl, naphthyl, thienyl, pyridyl or quinolinyl radical which can optionally be substituted by one or more substituents from the group consisting of halogen, OH, benzyloxy, C1-C4-alkyl, C1-C4-alkoxy, COOR1 where R1 is H or C1-C4-alkyl, by coupling of (S)-α-methylcysteine hydrochloride of the formula (II) with a nitrile of the formula (III) Ar—CN in which Ar is as defined above, or a corresponding C1-C4-alkyl imidate, in which (S)-α-methylcysteine hydrochloride of the formula (II) is reacted in a suitable solvent with a nitrile of the formula (III) or a corresponding C1-C4-alkyl imidate in the presence of a tertiary base at a pH of 6.5 to 10 at 50° C. up to the reflux temperature to give the corresponding thiazoline of the formula (I), and processes for the preparation of (S)-α-methylcysteine hydrochloride and its use for the preparation of thiazolines of the formula (I).

    摘要翻译： 制备式（I）的取代噻唑啉的方法，其中Ar是苯基，萘基，噻吩基，吡啶基或喹啉基，其可以任选地被一个或多个选自卤素，OH，苄氧基，C C 1 -C 4 - 亚烷基，C 1 -C 4 - 烷氧基，COOR 1 - 其中R 1是H或C 1 -C 4 - 烷基，通过将（S）-α-甲基半胱氨酸盐酸盐与 式（II）与式（III）的腈<？in-line-formula description =“In-line formula”end =“lead”？> Ar-CN <？in-line-formula description =“In- 其中Ar如上所定义，或其相应的C 1 -C 4 - 亚烷基亚氨酸酯，其中（S） - 式（II）的α-甲基半胱氨酸盐酸盐在合适的溶剂中与式（III）的腈或相应的C 1 -C 4 - 亚烷基亚氨基酯反应 在pH为6.5的叔碱存在下进行 至10℃，直到回流温度，得到相应的式（I）噻唑啉，以及制备（S）-α-甲基半胱氨酸盐酸盐的方法及其用于制备式（I）的噻唑啉的用途 一世）。