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- Title
A convenient method for the synthesis of roflumilast.
- Authors
Lin, Yan; Huang, Peijun; Liu, Shuai; Sima, Lifeng; Chen, Ligong; Wang, Donghua
- 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.
- Subjects
AMINOPYRIDINES; ORGANIC synthesis; BENZALDEHYDE; CYCLOPROPANE; SODIUM hydroxide; ALKYLATION; OXIDATION; POTASSIUM compounds
- Publication
Research on Chemical Intermediates, 2013, Vol 39, Issue 5, p2107
- ISSN
0922-6168
- Publication type
Article
- DOI
10.1007/s11164-012-0742-3