METHOD OF GRISEOLIC ACID DERIVATIVES SYNTHESIS Russian patent published in 1994 - IPC

FIELD: organic chemistry. SUBSTANCE: products: derivatives of griseolic acid of the general formula (1), where R - C₁-C₄-alkyl or aryl-C₁-C₄-alkyl; R¹ and R² - are similar or different, and every radical - hydrogen or carboxylic protective group. Reagent 1: , where R³ and R⁴ are similar or different, each of which is carboxylic protective group. Process of ring disruption is carried out in solvent at pH 6-8 retaining carboxylic groups, or at pH 11-13 removing carboxylic protective groups. Following recyclization of compound with disrupted ring is carried out at heating at 30-100 C in the solvent. Synthesized compounds are used in medicinal industry for synthesis of agents, which are able to inhibit activity of phosphodiesterases showing specificity for different cyclic nucleotides. EFFECT: improved method of synthesis. 1 tbl