CARBOPENEM DERIVATIVES, THEIR PHARMACEUTICALLY ACCEPTABLE SALTS AND HYDROLYZED IN VIVO ESTERS (VARIANTS), METHOD OF SYNTHESIS (VARIANTS), PHARMACEUTICAL COMPOSITION SHOWING ANTIBACTERIAL ACTIVITY, DERIVATIVES OF PYRROLIDINE-4-YLTHIOL AND PROTECTED DERIVATIVES OF PYRROLIDINE-4-YLTHIOL

摘要

FIELD: organic chemistry, antibiotics. SUBSTANCE: invention relates to carbapenems that can be used in medicine for therapeutic aims. Invention relates to the compound of the formula (I): where R means hydrogen; means hydroxymethyl or 1-hydroxyethyl; R and R mean hydrogen or -alkyl; R and R are similar or distinct and mean hydrogen, halogen, amino-, cyano-group, -alkyl, hydroxy-group, carboxy-group, -alkoxy-group, -alkoxycarbonyl, carbamoyl, -alkylcarbamoyl, di--alkylcarbamoyl, trifluoromethyl, sulfoacid group, -alkylamino, di---alkylamino-group, -alkanoylamino-group, -alkanoyl-[N--alkyl]-amino-group, -alkanesulfonamido-group, -alkylsulfinyl-group, -alkylthio-group and R -alkylsulfonyl-group at condition that no hydroxyl or carboxyl substituent at ortho-position, or its pharmaceutically acceptable salt or its ester hydrolyzed in vivo. Method of synthesis of compound of the formula (I) involves interaction of compound of the formula (VI) with compound of the formula (VII) . The claimed pharmcomposition shows antibacterial activity and contains compound of the formula (I) or its pharmaceutically acceptable salt, or its ester hydrolyzed in vivo. EFFECT: improved method of synthesis. 30 cl, 2 tbl