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Concise Synthesis of Key Intermediates of Pyriftalid and Paquinimod via Hydrogenation Method
Organic Process Research & Development ( IF 3.4 ) Pub Date : 2017-08-21 00:00:00 , DOI: 10.1021/acs.oprd.7b00177
Zhong Li 1 , Bing Li 2 , An-Jiang Yang 1 , Fu-Li Zhang 1
Affiliation  

An efficient and scalable synthesis of 7-amino-3-methylisobenzofuran-1(3H)-one (1) and 2-amino-6-ethylbenzoic acid (2) has been developed via a one-step catalytic hydrogenation. The triethylammonium salt of 2-acetyl-6-nitrobenzoic acid was used as the starting material and 1 was prepared in a biphasic solvent system of toluene/H2O, while 2 was obtained when the solvent was replaced with H2O. Intermediates 1 and 2 could be used to synthesize Pyriftalid and Paquinimod, respectively.

中文翻译:

氢化法简便合成丙酮酸和帕喹莫德的关键中间体

通过一步催化加氢,已开发出有效且可扩展的7-氨基-3-甲基异苯并呋喃-1(3 H)-一(1)和2-氨基-6-乙基苯甲酸(2)的合成方法。的2-乙酰基-6-硝基苯甲酸三乙基铵盐作为起始原料和1在甲苯中的两相溶剂体系制备/ H 2 O,而2时用H置换溶剂,得到2 O.中间体12可以分别用于合成Pyriftalid和Paquinimod。
更新日期:2017-08-21
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