The hitherto unknown (+)-and (Ϫ)-cis-2-aminocyclobutanols 6a,b and 7a,b, as well as the corresponding benzyloxycyclobutanamines 8a,b, have been synthesized by means of asymmetric reductive amination, with de values of 100% and ee values ranging from 96.9 to 99.8%. The relative cis configu-Second-generation asymmetric synthesis [1] remains one of the most popular methods for introducing chirality into potentially bioactive compounds. In pioneering work in this field, Overberger et al. [2] described the enantioselective synthesis of chiral primary amines by means of asymmetric reductive amination using (R)-(ϩ)-and (S)-(Ϫ)-1-phenylethylamine (PEA) as the chiral auxiliaries. In previous communications from this laboratory [3a] [3b] [3c] , we have reported on both enantio-and diastereoselective syntheses of various cyclic amines according to an analogous reaction sequence (Scheme 1). Scheme 1. Asymmetric reductive amination sequence Chiral α-amino alcohols have attracted much interest in recent years as substructures of very potent HIV-I protease inhibitors [4a] [4b] . Furthermore, chiral cyclic cis-α-amino alcohols are also of particular interest as effective ligands in asymmetric catalysis [5] [6a] and asymmetric synthesis [5] [6b] . This prompted us to devise a convenient synthesis of the optically active (ϩ)-and (Ϫ)-cis-2-aminocyclobutanols 6a,b.