Patent ID: 6566525
Filing Date: 2003-05-20
Classification: C07D,Y02P

Abstract:
A process for the preparation of N-substituted-hydroxycycloalkylamine derivatives represented by formula (1), which process comprises:(a) reacting; 1,2-dihydroxalkyl alcohol, represented by formula (2), with thionyl halide to produce an intermediate 1,2-cyclosulfinylalkyl halide represented by formula (3); and (b) cyclizing the intermediate 1,2-cyclosulfinylakyl halide represented by formula (3) with at least one nucleophilic compound selected from the group consisting of the amine compounds represented by formula (4): â€ƒwherein: * represents an asymmetric carbon atom; R1 is hydrogen or an amino-protecting group; and X is halogen; and wherein said compound 1 is further selected from the group consisting of compounds in which:where m=1, n=1, R2=OH, and R3=H; where m=2, n=1, R2=H, and R3=CH2OH; where m=2, n=2, R2=OH, and R3=H; and where m=3, n=2, R2=H, and R3=CH2OH.