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 Russian patent published in 1998 - IPC

Abstract RU 2117659 C1

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; R2 and R3 mean hydrogen or -alkyl; R4 and R5 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 R3-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

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RU 2 117 659 C1

Authors

Majkl Dzhon Betts

Garet Mors Dehvis

Majkl Lingard Svejn

Dates

1998-08-20Published

1993-02-02Filed