A convenient method for the synthesis of roflumilast

…, P Huang, S Liu, L Sima, L Chen, D Wang

文献索引：Lin, Yan; Huang, Peijun; Liu, Shuai; Sima, Lifeng; Chen, Ligong; Wang, Donghua Research on Chemical Intermediates, 2013 , vol. 39, # 5 p. 2107 - 2113

全文：HTML全文

被引用次数: 5

摘要

Abstract A convenient synthetic method has been developed for the synthesis of roflumilast from 4-difluoromethoxy-3-hydroxybenzaldehyde and bromomethyl cyclopropane via O- alkylation, oxidation and N-acylation. With sodium hydroxide as alkali in the last step, the total yield of roflumilast can be up to 68.3% and the purity of the target product reached 99.2%. It was obvious that sodium hydroxide showed more economic advantage for scale- ...