57320-63-5Relevant articles and documents
A preparation method of roflumilast
-
Paragraph 0102-0103; 0108-0109; 0114-0115; 0120-0121, (2019/04/13)
The invention discloses a method for preparation of roflumilast, comprises the following steps: 4 - (methoxy) benzoic acid chlorization reaction to obtain 4 - (methoxy) benzoyl chloride; with 3, 5 - dichloro - 4 - aminopyridine by amidation reaction to obtain N - (3, 5 - dichloro - 4 - pyridyl) - 4 - (methoxy) benzamide; then by Vismeier reaction to obtain N - (3, 5 - dichloro - 4 - pyridyl) - 4 - (methoxy) - 3 - formyl-benzoyl; through the Baeyer - villiger - hydrolysis reaction to obtain N - (3, 5 - dichloro - 4 - pyridyl) - 4 - (methoxy) - 3 - hydroxy benzoyl; then with the [...] yl cyclopropane ether to obtain roflumilast. The invention starting raw material is cheap, the reaction conditions are mild and controllable, synthetic route green environmental protection, high yield, the prepared Roflumilast purity is good.
NOVEL PYRROLIDINE DERIVED BETA 3 ADRENERGIC RECEPTOR AGONISTS
-
Page/Page column 33, (2015/04/22)
The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of β3-adrenoceptor.