FIELD: organic chemistry. SUBSTANCE: synthesis of proposed compound can be carried out by two variants I: a) from 2,2-dimethyl-4-morpholino-2,3-dihydro-6H-pyrane, Br2 in chloroform medium at stirring and cooling up to -15 C (above 1 hr) and at 20 C (2.5 hr); b) from prepared product with thiourea in ethanol medium at boiling (8 hr); or II: by reaction of 2,2-dimethyltetrahydropyrane-4-one, sulfur, cyanamide and diethylamine in ethanol medium at boiling and stirring reaction mixture (1.5 hr). The yield of the end product is 42.6-53.5%; m. p. is 163-164 C (in ethanol); empirical formula is C8H12N2OS. The end product has toxicity LD50 = 760 mg/kg, anticorazol activity at the dose ED50 = 35 mg/kg. Neurotoxic effect (coordination injury in mice) is observed at the dose 310 mg/kg). Under condition of conflict situation water drinking is increased by 3-fold at the dose of proposed compound as compared with control. Known phazepam under the same conditions increases water drinking by 38-fold. EFFECT: enhanced activity of product. 2 tbl
Title |
Year |
Author |
Number |
2-METHYLAMINO-4-OXO-3,6,6-TRIMETHYL-5,6-DIHYDRO-8H-PIRANO[4′,3′:4,5]TIENO[2,3-<D>]PYRAMIDIN OR ITS SALTS POSSESSING ANTICONVULSIVE ACTIVITY |
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