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以自制的(R,R)-Salen-Co(Ⅲ)·BF3(4)催化外消旋?-萘基缩水甘油醚(2)的水解动力学拆分,获得高光学纯度的(S)-?-萘基缩水甘油醚[(S)-2]和(R)-3-(?-萘氧基)-1,2-丙二醇(5),并采用Sharpless的“一锅法”将5转化为(R)-2。(R)-2和(S)-2分别与1-(2-甲氧基苯基)哌嗪(3)反应得到(R)-和(S)-萘哌地尔,ee值98%。
(S) - (2) was catalyzed by (R, R) -Salen-Co (Ⅲ) · BF3 (4) catalyzed hydrolysis of racemic-naphthyl glycidyl ether (2) ? -naphthyl glycidyl ether [(S) -2] and (R) -3 - (? - naphthyloxy) -1,2-propanediol (5) 5 into (R) -2. Reaction of (R) -2 and (S) -2 with 1- (2-methoxyphenyl) piperazine (3) gave (R) - and (S) -nappepodil with ee values of 98%.