| 摘要 |
<p>1. A process for the preparation of cycloalkylpropanolamines corresponding to the general formula I : see diagramm : EP0037777,P10,F2 wherein A represents a non aromatic, cyclic carbon radical, containing at least one ring, R1 represents an alkyl or acyl radical, R2 represents hydrogen or an alkyl radical, B represents a methylene radical, m represents 0, 1 or 2, and when m does not represent O, R1 may represent hydrogen, R represents an alkyl, alkenyl, alkynyl, or an aralkyl radical, and when R represents an unsaturated radical, R1 may represent hydrogen, characterised in that epichlorohydrin is reacted with an alcohol corresponding to formula IV : see diagramm : EP0037777,P10,F3 wherein R1 , R2 , A, B and m are as defined in formula (I), in the presence of a base in aqueous solution and in the presence of a catalyst of the quaternary ammonium type, to obtain the intermediate epoxide corresponding to formula II : see diagramm : EP0037777,P10,F4 which is reacted in a solvent with a primary amine corresponding to formula III : R-NH2 wherein R is as defined in formula I, to obtain the cyloalkyl propanolamine derivatives corresponding to formula (I).</p> |
