Practical preparation of trimethoprim: a classical antibacterial agent

…, JA Jiang, HW Liu, DH Liao, XY Wei

Index: Ji, Ya-Fei; Jiang, Jian-An; Liu, Hong-Wei; Liao, Dao-Hua; Wei, Xian-Yong Synthetic Communications, 2013 , vol. 43, # 11 p. 1517 - 1522

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Citation Number: 5

Abstract

Supplemental materials are available for this article. Go to the publisher's online edition of Synthetic Communications® to view the free supplemental file. ... An efficient, simple, and mild preparation of the classical antibacterial agent trimethoprim (1) was achieved in 85% overall yield from 3,4,5-trimethoxybenzaldehyde (2). First, the addition of propenenitrile (3) with dimethylamine almost quantitatively afforded 3-dimethylaminopropanenitrile (7). Then, by condensation ...