1,4-DIHYDROPYRIDINE DERIVATIVES OR THEIR HYDROCHLORIDES SHOWING ANTAGONISTIC PROPERTIES WITH RESPECT TO CALCIUM IONS Russian patent published in 1995 - IPC

Abstract RU 2036922 C1

FIELD: organic chemistry. SUBSTANCE: product: derivatives of 1,4-dihydropyridine or their hydrochlorides of the formula (I) where R1-C1-C3-alkyl; R2 - methyl or benzyl; R3 - formyl, picolyl, 4-fluorobenzyl or 2-thienylmethyl. Reagent 1: 2,3-methylenedihydroxybenzaldehyde. Reagent 2: acetoacetic acid ester of the formula (II) CH3-C(O)-CH2-C(O)-OA where A - group R1 or -CH2-CH2-NR2R3. Reagent 3: alpha-acetyl-beta-(2,3-methylenedihydroxyphenyl)-acrylic acid ester. Reagent 4: 3-aminocrotonic acid ester of the formula (III) NH2-C(CH3)CH-C(O)-OB where B - R1 or CH2-CH2-NR2R3 at condition that "B" is different from "A". Reaction conditions: after interaction reaction the end product is isolated in the free form or as hydrochloride. Compounds of the formula (I) as aqueous-spirituous solution at the dose 0.1 mg/ml or at intravenous route of administration show high activity against contractions of rat aorta induced KCl: value ИК50 is 5.58(+ or -1.2)*10 mM, ЛД50 = 30-80 mg/kg. Synthesized compounds were used in medicine. EFFECT: improved method of synthesis, increased effectiveness of products.

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RU 2 036 922 C1

Authors

Karlos Fernandes Torikha[Es]

Khoakin Al'Varo Galiano Ramos[Es]

Dates

1995-06-09Published

1992-03-31Filed