陈秀英, 余一成, 王其灼, 陈永华, 张嘉生, 任秀娟. 胍乙啶的合成J. 药学学报, 1964, 11(4): 281-284.
引用本文: 陈秀英, 余一成, 王其灼, 陈永华, 张嘉生, 任秀娟. 胍乙啶的合成J. 药学学报, 1964, 11(4): 281-284.
CHENG SU-YING YU YI-CHENG WANG CHI-CHO CHENG YUN-HUA CHANG CHAI-SHENG REN SU-DRAN, . THE PREPARATION OF GUANETHIDINEJ. Acta Pharmaceutica Sinica, 1964, 11(4): 281-284.
Citation: CHENG SU-YING YU YI-CHENG WANG CHI-CHO CHENG YUN-HUA CHANG CHAI-SHENG REN SU-DRAN, . THE PREPARATION OF GUANETHIDINEJ. Acta Pharmaceutica Sinica, 1964, 11(4): 281-284.

胍乙啶的合成

  • 摘要: 提供了降压药胍乙啶(Ⅷ)的工业生产法。以鉄屑替代Raney-Ni或电解法还原,制成原料环庚酮(Ⅰ)。Mull原合成路线中的二步采用氫化鋁鋰的反应,分别改用电解法和Gabriel法来完成。

     

    Abstract: An industrial method for the preparation of the antihypertensive drug guanethidine (Ⅷ) has been described. The manufacture of the raw material cycloheptanone (Ⅰ) via 1-nitromethylcylohexanol was accomplished by the conventional reduction by means of iron filings and hydrochloric acid. This modification gave results in overall yield (55—60% against the nitro compound) compared favourably with those obtained by the reported procedures, such as catalytic reduction or electrolytic reduction. It offers advantages of cheapness, rapidity, simplicity and industrial adaptibility. Electrolytic reduction of the appropriate thiolactam (Ⅲ) gave cycloheptamethylenimine (Ⅳ), which in turn through the Gabriel synthesis led to 2-(octahydro-1-azocinyl)ethylamine (Ⅶ).

     

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