'-(N-ACYLAMINO) ALKYLPHOSPHORYL ETHANOLAMINES, PROCESS FOR PREPARING THEM, PHARMACEUTICAL COMPOSITIONS AINING THEM, AND THEIR USES

摘要

New .omega.-(N-acylamino)alkylphosphoryl ethanolamines and their pharmaceutically acceptable acid addition salts having superior renin-inhibitory activities, antihypertensive activities alkylphosphoryl ethanolamines are prepared by (1) reacting an .omega.-(N-acylamino) alkanol with a 2-(N-substituted amino)ethyl phosphate or its derivative, hydrolyzing the resulting product or splitting off the phosphoric acid-protective group of the resulting product thereby to form an .omega.-(N-acylamino) alkyl-2-(N-substi-tuted amino) ethyl phosphate, and splitting off the aminoprotective groups of the resulting phosphate, or (2) reacting an .omega.-(N-acylamino) alkanol with a phosphorus oxyhalide, reacting the resulting .omega.-(N-acylamino)alkyl dichlorophosphate with a 2-(N-substituted amino) ethanol, hydrolyzing the reaction product to from an .omega.-(N-acylamino)alkyl 2-(N-substituted)ethyl phosphate, and splitting off the amino-protective groups of said phosphate.