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反应停(Ⅰ)具有致畸的副作用。近来由于其在麻风病化学治疗方面的价值而受到日益重视,但其致畸原理一直不清楚。1981年,Koch 报道在(Ⅰ)的戊二酰亚胺部分减少一个 CH_2基团形成的低反应停(Ⅱ)的致畸毒性较(Ⅰ)高。Fickentscher进而设想在(Ⅰ)的戊二酰亚胺部分增加一个CH_2基团使其成为高反应停(Ⅲ),将具有(Ⅰ)的催眠镇静作用而无致畸的副作用。本文以 D(+)-和L(-)-α-氨基己内酰胺为原料经两步合成得到高产率(Ⅲ)的异构
Reaction stop (Ⅰ) has teratogenic side effects. Recently, due to its value in the treatment of leprosy has received increasing attention, but its teratogenic principle has not been clear. In 1981, Koch reported that the teratogenicity of (Ⅱ) teratogenicity induced by the reduction of one CH_2 moiety in the glutarimide moiety of (I) was higher than that of (I). Fickentscher further envisions adding a CH 2 group to the glutarimide moiety of (I) to make it a hyperresponsive (III) moiety that will have the hypnotic sedation of (I) without teratogenic side effects. In this paper, D (+) - and L (-) - α-amino caprolactam as raw materials were synthesized in two steps by high yield (Ⅲ)