富马酸贝达喹啉(bedaquiline fumarate,1),化学名为(1R,2S)-1-(6-溴-2-甲氧基喹啉-3-基)-4-二甲胺基-2-(萘-1-基)-1-苯基-2-丁醇富马酸盐(1∶1),由美国Johnson&Johnson公司开发,可通过抑制ATP合成酶,来抑制结核分枝杆菌。美国FDA于2013年批准其上市,临床用于治疗对多种药物耐药的成人结核患者[1-3]。本文按起始原料及构建次序的不同,总结1的合成方法如下(图1)。A法:N-乙酰基-4-溴苯胺(4)在三氯氧磷/ Bedaquiline fumarate (1) with the chemical name (1R, 2S) -1- (6-bromo-2-methoxyquinolin-3-yl) 2- (Naphthalen-1-yl) -1-phenyl-2-butanol fumarate (1: 1), developed by Johnson & Johnson, USA, inhibits M. tuberculosis by inhibiting ATP synthase. The US FDA approved its listing in 2013 for clinical use in the treatment of adult TB patients resistant to multiple drugs [1-3]. In this paper, according to the different starting materials and the order of construction, the synthesis method of summary 1 is as follows (Figure 1). Method A: N-acetyl-4-bromoaniline (4) in phosphorus oxychloride /