An alternative route for synthesis of o-trifluoroacetylanilines as useful fluorine-containing intermediates

作者：Zhu Lingjian; Miao Zhenyuan^*; Sheng Chunquan; Yao Jianzhong; Zhuang Chunlin; Zhang Wannian

来源：Journal of Fluorine Chemistry, 2010, 131(7): 800-804.

DOI：10.1016/j.jfluchem.2010.04.002

• Fluorine-containing compound
• o-Trifluoroacetylaniline
• Synthesis
• Trifluoroacetic anhydride (TFAA)

A series of o-trifluoroacetyl aniline derivatives were synthesized in three steps. In this method, we first utilized trifluoroacetic anhydride to introduce trifluoroacetyl group to the ortho position of aniline with higher yield than that of some previously reported methods. In addition, the procedure is shown to be highly regiospecific. This type of compounds can be used as the key intermediates in the preparation of a variety of inhibitors of HIV reverse transcriptase which is an important pharmacological target of many anti-AIDS agents.

• 出版日期2010-7
• 单位中国人民解放军第二军医大学