Process for the preparation of a...

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C - Chemistry, Metallurgy

07

C

260/603.3, 260/5

C07C 233/00 (2006.01)

Patent

CA 1248967

ABSTRACT There are disclosed a process for producing (-)-5- (R)-1-hydroxy-2-[(R)-1-methyl-3-phenylpropyl amino- ethyl salicylamide and its acid addition salts in high yields which does not require chromatography, and impor- tant intermediates in this process. The process is stereoselective for the desired (R,R) amine; a preferred embodiment includes the steps of (1) reaction of an N-[(R)-protected]-(R)-1-methyl-3-phenyl- propylamine with a 4-0-protected 2-bromo-3-carbamoyl-ace- tophenone to produce the corresponding R,R-glycyl-benza- mide, (2) reduction to produce a mixture of S,R,R;R,R,R- -hydroxybenzamides, (3) removal of the protecting groups, (4) resolution of the deprotected product and, if de- sired, conversion to the free R,R -amine or to another salt. In this process, the selection of particular N-pro- tecting groups has a very favourable effect, especially in steps (2) and (3).

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