1. A convenient method for the synthesis of roflumilast.
- Author
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Lin, Yan, Huang, Peijun, Liu, Shuai, Sima, Lifeng, Chen, Ligong, and Wang, Donghua
- Subjects
AMINOPYRIDINES ,ORGANIC synthesis ,BENZALDEHYDE ,CYCLOPROPANE ,SODIUM hydroxide ,ALKYLATION ,OXIDATION ,POTASSIUM compounds - 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-up production than sodium hydride or potassium tert-butoxide. [ABSTRACT FROM AUTHOR]
- Published
- 2013
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