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A Cu (I) catalyzed large scale synthesis of an antipsychotic drug substance Clozapine with new precursor 2-chloro benzoic acid
Arabian Journal of Chemistry ( IF 6 ) Pub Date : 2020-07-01 , DOI: 10.1016/j.arabjc.2020.05.003
S. Venkat Rao

Abstract Development of an economic and commercial manufacturing process for an anti-psychotic drug substance clozapine with an alternative key starting material (2-chloro benzoic acid) in the place of literature reported key starting material Anthranilic acid. To avoid narcotic key starting materials usage in drug substances the author invented a commercially available raw material 2-chlorobenzoic acid, which reacts with another key starting material 4-chloro-1, 2-diamino benzene. This reaction proceeds through Ullman reaction to produce multi scale level Clozapine which quality meets the ICH requirements.

中文翻译:

A Cu (I) 催化抗精神病药物氯氮平与新前体 2-氯苯甲酸的大规模合成

摘要 用替代的关键原料(2-氯苯甲酸)代替文献报道的关键原料邻氨基苯甲酸,开发了一种经济和商业化的抗精神病药物氯氮平生产工艺。为避免在原料药中使用麻醉性关键原料,作者发明了一种市售原料2-氯苯甲酸,该原料与另一种关键原料4-氯-1,2-二氨基苯反应。该反应通过Ullman反应进行,生产出质量符合ICH要求的多尺度水平的氯氮平。
更新日期:2020-07-01
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