3-Amino-1-(diphenylmethyl)azetidine → (2S)-N2-(1-benzhydryl-3-azetanyl)-1-(1,3-benzoxazol-2-yl)-2-piperidinecarboxamide

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Reaction Steps

The title compound was prepared by a similar method to Example 1 from (2S)-1-(1,3-benzoxazol-2-yl)-2-piperidinecarboxylic acid [see Preparation 3] and 1-benzhydryl-3-azetanamine [see J. Med. Chem. (1977), 21(1), 78-82]. The crude product was purified by column chromatography on silica gel eluting with a solvent gradient of 80:20 changing to 60:40, then 50:50, by volume, hexane:ethyl acetate to afford (2S)-N2-(1-diphenylmethyl-3-azetidinyl)-1-(1,3-benzoxazol-2-yl)-2-piperidinecarboxamide as a white foam.

Provenance & Evidence