.omega.-(n-acylamino) alkylphosphoryl ethanolamines, process...

C - Chemistry – Metallurgy – 07 – F

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260/460.5

C07F 9/09 (2006.01)

Patent

CA 1052810

ABSTRACT OF THE DISCLOSURE 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 result- ing product thereby to form an .omega.-(N-acylamino) alkyl-2-(N-substi- tuted amino) ethyl phosphate, and splitting off the amino- protective 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. - 1 -

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