abstract |
*FORMULA* PROCEDURE FOR THE PREPARATION OF ALPHA-HALOMETYL AMINE DERIVATIVES OF FORMULA (I), AND THEIR INDIVIDUAL PHARMACEUTICALLY ACCEPTABLE SALTS AND OPTICAL ISOMERS, WHERE Y IS FCH2-, F2CH-, F3C-; R1 MAY BE HYDROGEN OR OTHER TYPES OF RADIALS. DEPENDING ON THE RADIALS OF AND HOW IT IS PROCEEDED TO OBTAIN THEM, R3, R4, R5, R''4 AND R6 MAY BE DIFFERENT TYPES OF RADIALS. ONE OF THE METHODS IS TO CHEMICALLY AND CATALYTICLY REDUCE A DERIVATIVE OF PHENYL HALOMETHYL KETONE, TREATED WITH AN IMIDE, WITH A PHOSPHINE AND WITH DIETHYL AZODICARBOXYLATE IN AN APPROPRIATE SOLVENT. ANOTHER METHOD IS TO TREAT AN ALKYL MALONIC ACID DIESTER WITH A STRONG BASE IN A SUITABLE APROTIC SOLVENT, WHICH GENERATES A CARBANION THAT IS ALKYLED WITH A CERTAIN COMPOUND AND SUBSEQUENTLY THE DESIRED COMPOUND IS OBTAINED. OTHER METHODS ARE ALSO CLAIMED. THESE COMPOUNDS HAVE PHARMACOLOGICAL PROPERTIES. |