| 摘要 |
Roflumilast and new key intermediates therefor are prepared by processes involving use of carbonylation technology. Good overall yields can be achieved using available starting materials. The starting material for the process can be catechol, an o-R1-phenol an o-R1-p-X-phenol, or a 1-X-3-R1-4-R2-benzene, where R1, is a C1-6alkoxy, C3-7 cycloalkoxy, C3-7 cycloalkylmethoxy, or benzyloxy group, or a C1-4 alkoxy group which his completely or partially substituted by fluorine; R2 is a C1-4 alkoxy group which his completely or partially substituted by fluorine; and X is C1, Br, or I. |
