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    • 1. 发明授权
    • Process for the preparation of substituted thiazolines and their intermediates
    • 制备取代噻唑啉及其中间体的方法
    • US06894170B2
    • 2005-05-17
    • US10270324
    • 2002-10-15
    • Sylvia KrichAlexander RiederFerdinand HeuGerhard Steinbauer
    • Sylvia KrichAlexander RiederFerdinand HeuGerhard Steinbauer
    • C12P41/00C07B55/00C07B57/00C07C319/02C07C319/28C07C323/58C07D277/12C07D417/04C07D277/10
    • C07D417/04C07C319/02C07D277/12C07C323/58
    • 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).
    • 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)。
    • 2. 发明申请
    • Process for the preparation of substituted thiazolines and their intermediates
    • 制备取代噻唑啉及其中间体的方法
    • US20050101782A1
    • 2005-05-12
    • US11011110
    • 2004-12-15
    • Sylvia KrichAlexander RiederFerdinand HeuGerhard Steinbauer
    • Sylvia KrichAlexander RiederFerdinand HeuGerhard Steinbauer
    • C12P41/00C07B55/00C07B57/00C07C319/02C07C319/28C07C323/58C07D277/12C07D417/04
    • C07D417/04C07C319/02C07D277/12C07C323/58
    • 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).
    • 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)。