Procedure for the preparation of N-cyclopropyl-4-fluoroanilines of formula I. By selective reaction of II with cyclopropylamine, piperazines or pyrrolidines, III is obtained. Its acetylation and reduction yields IV which by de-amination leads to I. R¹ is hydrogen, chlorine or methyl; R², hydrogen, halogen, methyl, a piperazinyl or a pyrroledinyl; R³, hydrogen, halogen, hydroxyl or trifluoromethyl; and R⁴, hydrogen, nitro, hydroxyl or amino.
The compounds of formula I are of interest on account of their application to the preparation of quinolone group antibiotics.
制备式I的
N-环丙基-4-氟苯胺的过程。通过将II与
环丙基胺、
哌嗪或
吡咯烷选择性反应,得到III。对其进行乙酰化和还原得到IV,再经去
氨基化得到I。其中,R¹为氢、
氯或甲基;R²为氢、卤素、甲基、
哌嗪基或
吡咯烷基;R³为氢、卤素、羟基或三
氟甲基;R⁴为氢、硝基、羟基或
氨基。式I的化合物因其在喹诺
酮类抗生素制备中的应用而备受关注。