| 摘要 |
A side chain -OCH2CHOHCH2NHR2 is fixed to a hydroxythiochroman of formula: <IMAGE> by a 2-stage synthesis, a) reaction with a glycerol halohydrin in basic medium and b) reaction of the 2,3-dihydroxypropoxythiochroman thus formed with an amine R2NH2 in the presence of an aminotriphenylphosphonium halide. The compounds (I) thus obtained and their salts are known as beta -blocking agents and used, especially, in the treatment of disorders of the cardiac rhythm. Compared with the prior process starting from the same compounds (II) and ending in the same compounds (I), the new process requires shorter reaction times and a reduced quantity of the amine R2NH2, which makes possible a selective amination of the primary alcohol functional group. |
