专利号:US-6566525-B1 优先权日:1998-09-17 标 题:Preparation of N-substituted-hydroxycycloalkylamine derivatives 发明人:KIM SEONG JIN; KIM KEON IL; YANG KYOUNG YOUL 权利人:SAMSUNG FINE CHEMICALS CO LTD 摘要:A process for the preparation of N-substituted-hydroxycycloalkylamine derivatives, that are useful intermediates for the synthesis of various organic chemicals including pharmaceutical and agrochemical compounds, represented by formula (1), by reacting a 1,2-dihydroxalkyl alcohol, represented by the following formula (2), with a thionyl halide to produce an intermediate 1,2-cyclosulfinylalkyl halide represented by the following formula (3); and then cyclizing that intermediate with an amine compounds represented by the following formula (4).In the above structural formuli, * represents an asymmetric carbon atom; R1 is hydrogen or an amino-protecting group; m is an integer of 1-3; and X is halogen. The reactant compounds as well as the compounds made according to this invention have the following substitution pattern:n=1, R2=OH, R3=H and m=1; n=1, R2=H, R3=CH2OH and m=2;n=2, R2=OH, R3=H; and m=2; and n=2, R2=H, R3=CH2OH and m=3.
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