Process development and large-scale synthesis of a PDE4 inhibitor
An efficient, scalable synthesis of the PDE4 inhibitor, 6-[1-methyl-1-(methylsulfonyl)ethyl]-8-(3-{(E)-2-(3-methyl-1,2,4-oxadiazol-5-yl) -2-[4-(methylsulfonyl)phenyl]vinyl}phenyl)-quinoline benzenesulfonate (10) is described. The synthesis is highly conve
Conlon, David A.,Drahus-Paone, Antoinette,Ho, Guo-Jie,Pipik, Brenda,Helmy, Roy,McNamara, James M.,Shi, Yao-Jun,Williams, J. Michael,Macdonald, Dwight,Deschenes, Denis,Gallant, Michel,Mastracchio, Anthony,Roy, Bruno,Scheigetz, John
p. 36 - 45
(2012/12/21)
Discovery of a substituted 8-arylquinoline series of PDE4 inhibitors: Structure-activity relationship, optimization, and identification of a highly potent, well tolerated, PDE4 inhibitor
The discovery and SAR of a new series of substituted 8-arylquinoline PDE4 inhibitors are herein described. This work has led to the identification of several compounds with excellent in vitro and in vivo profiles, including a good therapeutic window of em
An efficient and high-yielding one-pot synthesis of 1,2,4-oxadiazoles from carboxylic acids and amidoximes is described. Activation of the carboxylic acid using hydroxybenzotriazole (HOBt) and EDC/HCl followed by reaction with an amidoxime generates an oxime ester. Without isolation, the oxime ester is dehydrated to give the oxadiazole ring.
Pipik, Brenda,Ho, Guo-Jie,Williams, J. Michael,Conlon, David A.
p. 1863 - 1870
(2007/10/03)
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