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瑞波西汀(reboxetine),化学名为2-[(2-乙氧基苯氧基)苯甲基]吗啉,由Pharmacia&Upjohn公司开发,1997年在英国首次上市,临床用于治疗抑郁症[1,2]。(S,S)-瑞波西汀(1)在其4种对映体中的活性最高,是(R,R)-瑞波西汀药效的24倍[3],且在治疗神经性疼痛及其他疾病方面也表现出一定的疗效[4]。1的传统制备方法是通过拆分消旋体得到[5-8],总收率低于10%[9],严重制约了临床使用,
Reboxetine, chemically named 2 - [(2-ethoxyphenoxy) benzyl] morpholine, was developed by Pharmacia & Upjohn and was first introduced in the UK in 1997. It is clinically used to treat depression [1 ,2]. (S, S) -reboxetine (1) has the highest activity among its four enantiomers, which is 24 times more potent than (R, R) -reboxetine [3] and has shown efficacy in the treatment of neuropathic pain and Other diseases also showed some effect [4]. 1 traditional preparation method is obtained by the resolution of racemates [5-8], the total yield of less than 10% [9], severely restricted the clinical use,