Mannich Reaction of Acetaminophen

黃文鑫(Wen-Hsin Huang) ； 李小鳳(Hsiao-Feng Lee) ； 李安榮(An-Rong Lee)

《The Chinese Pharmaceutical Journal》 54卷6期 (2002/12) Pp. 485-490

https://doi.org/10.7019/CPJ.200212.0485

並列摘要

A series of acetaminophen derivatives 8-13 as a new class of phosphodiesterase (PDE) inhibitors was synthesized from acetaminophen (7) by Mannich reaction. Depending on the amount of ammines used, the products were found to be either mono- or di-substituted, which is in contrast to the exclusive mono-substitution in oxindoles 3 and 4 reported previously. An energy-minimization study showed that their different behaviors are due primarily to steric environments.

並列關鍵字

Acetaminophen ； Phosphodiesterase inhibitor ； Computational study ； Non-steroidal cardiotoDics ； Mannich bases