DERIVATIVES OF N-(PYRROLO[2,3-D]PYRIMIDINE-3-YLACYL)-GLUTAMIC ACID OR THEIR TAUTOMERS OR THEIR PHARMACEUTICALLY ACCEPTABLE SALTS AND A METHOD OF THEIR SYNTHESIS Russian patent published in 1996 - IPC

FIELD: organic chemistry. SUBSTANCE: products: derivatives of N-(pyrrolo-[2,3-d] pyrimidine-3-ylacyl)-glutamic acid of the general formula where R₁ - unsubstituted 1,4-phenylene or substituted with chlorine or fluorine, thiendiyl, furandiyl, cyclohexandiyl or C₂-C₄-alkanediyl; R₂ - hydrogen, methyl of hydroxymethyl; R₃ - hydrogen, C₁-C₆-alkyl or amino-group; * - S-configuration of labeled carbon atom, or their tautomers or pharmaceutically acceptable salts. Reagent 1: compound of the formula where X - COOR′ or

Z - hydrogen or Z together with -carbon-carbon bond; R′ - hydrogen or protective group for carboxyl; and * have values indicated above; - independently of Z - hydrogen, methyl, hydroxymethyl or protected hydroxymethyl; - hydrogen, C₁-C₆-alkyl, amino-group or lower alkanoylamino-group which is subjected for catalytic hydrogenation and compound of the formula

is synthesized where and * have indicated values; X - COOR′ which is added to the reaction with protected glutamic acid, and compound is synthesized where
.

Compound is subjected for acidic or alkaline hydrolysis or both for conversion of R′-carboxy-protected group to hydrogen or salt, - protected hydroxymethyl to hydroxymethyl, -alkanoylamino-group to amino-group. Synthesized compounds were used in medicine. EFFECT: improved method of synthesis. 5 cl, 6 tbl