Journal of Chemical Research

An improved synthesis of a β-blocker celiprolol hydrochloride

L Ji, XY Mao, C Qian, XZ Chen

文献索引：Ji, Li; Qian, Chao; Chen, Xin-Zhi; Mao, Xiao-Yuan 2011 , vol. 35, # 11 p. 640 - 643,4

被引用次数: 0

摘要

Celiprolol hydrochloride, a β-blocker drug, has been synthesised from 4- chloronitrobenzene. The route involved hydrolysis of the chloride and acetylation of the phenol, reduction of the nitro group, and acylation of theamine. This was followed by Fries rearrangement of the acetyl group, Williamson etherification with epichlorohydrin, followed by opening of the epoxide ring and salt formation. The overall yield of celipropol was 39.1 ...

~90%

~80%

~87%

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