| 摘要 |
<p>The present invention relates to the preparation of N-substituted-hydroxycycloalkylamine derivatives and more particularly, to the method for synthesis of N-substituted-hydroxycycloalkylamine derivatives represented in formula (1), regioselectively in high yield via 1,2-cyclosulfinyl halide as an intermediate from the 1,2-dihydroxyalkyl alcohol as a starting material. In said formula, * represents an asymmetric carbon; R1 is hydrogen, linear alkyl, branched alkyl, or cycloalkyl containing 1∩10 carbon atoms or typical amino-protecting groups such as aromatic hydrocarbons; n is 1 or 2, with the proviso that if n=1 then R2=OH and R3=H or R2=H and R3=CH2OH, if n=2 then R2=OH and R3=H or R2=H and R3=CH2OH.</p> |
