The present invention relates to a process for the preparation of enantiomerically and diastereomerically enriched cyclobutane amines and amides by reacting (a) cyclopropylcarbonitrile to a cyclopropylcarbaldehyde, (b) further reacting to a cyclobutanone, or (d′) further reacting to an enamide, (c) further reacting to enantiomerically and diastereomerically enriched cyclobutane amines, or (d) further reacting to an enamide and (e) to an enantiomerically and diastereomerically enriched cyclobutylamide to obtain (f) an enantiomerically and diastereomerically enriched cyclobutane amine, and (g) further reacting to an enantiomerically and diastereomerically enriched cyclobutane amide.
本发明涉及一种制备对映体和非对映异构体富集的
环丁烷胺和酰胺的工艺,该工艺通过(a)
环丙基甲腈与
环丙基甲醛反应,(b)进一步与
环丁酮反应,或(d′)进一步与烯酰胺反应,(c)进一步与对映体和非对映异构体富集的
环丁烷胺反应、或(d)与烯酰胺和(e)与对映体和非对映异构体富集的
环丁基酰胺进一步反应,得到(f)对映体和非对映异构体富集的
环丁烷胺,和(g)与对映体和非对映异构体富集的
环丁烷酰胺进一步反应。