2-Amino-1-methylcyclopentanol hydrochloride → 2-Chloro-4-{[(1r,2r)-2-Hydroxy-2-Methylcyclopentyl]amino}-3-Methylbenzonitrile

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Reaction Steps

2-Chloro-4-[[2-hydroxy-2-methyl-cyclopentyl]amino]-3-methyl-benzonitrile is prepared essentially as described in Example 1 using 2-amino-1-methyl-cyclopentanol, hydrochloride and 2-chloro-4-fluoro-3-methyl-benzonitrile. The crude material was purified using silica gel chromatography (25-55% EtOAc/hexane) to obtain Diastereomer 1 (0.54 g) and Diastereomer 2 (1.56 g). Diastereomer 2 is assigned trans configuration based on co-crystal with AR.

Provenance & Evidence