| 摘要 |
There is disclosed a multistep process for producing (-)-5-[(_R)-1-hydroxy-2-((_R)-1-methyl-3-phenyl-propyl)aminoethyl]sali cylamide in high yields which does not require chromatography. The process is stereoselective for the desired products starting with the reaction of D-(+)-alpha-methylbenzylamine with benzylacetone followed by reduction of the resulting Schiff's base to form an amine as an _R,_R: _R,_S diastereomeric mixture, resolution of the mixture to obtain the _R,_R stereoisomer as a salt, conversion to a free base, reaction of the _R,_R free base with an _O-protected alpha-bromo-3-carbamoyl-acetophenone to produce the corresponding _R,_R-ketobenzamide, reduction to produce a mixture of _S,_R,_R;_R,_R,_R hydroxybenzamide, removal of the protecting groups, resolution of the deprotected product and then conversion to the free _R,_R-amine.
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