Phenylalkylaminoethylsalicylamide, its preparation and...

Details Phenylalkylaminoethylsalicylamide, its preparation and... Phenylalkylaminoethylsalicylamide, its preparation and...

C - Chemistry, Metallurgy

07

C

260/550.8

C07C 233/00 (2006.01) A61K 31/60 (2006.01)

Patent

CA 1151211

ABSTRACT The (R,R) optical isomer of labetalol, namely 5-{ (R)- -l-hydroxy-2-[(R)-l-methyl-3-phenylpropyl)amino]ethyl} sali- cylamide, and its pharmaceutically acceptable acid addi- tion salts, in a state substantially free of the correspon- ding (R,S), (S,R) and (S,S) optical isomers, are novel com- pounds with favourable therapeutic properties in compari- son with labetalol. They can be used in particular in the treatment of hypertension. The novel (R,R) optical isomer and its pharmaceutically acceptable acid addition salts can be prepared by removal of the protecting groups from an N,O-protected (R,R) opti- cal isomer or acid addition salt thereof, wherein the ba- sic nitrogen atom and the phenolic hydroxy group are pro- tected, preferably by hydrogenolytic removal of hydrogeno- lysable groups.

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