PROCESS FOR OBTAINING 1,2,4-OXADIAZINE DERIVATIVES

5,6-Dihydro-4H, 1,2,4-oxadiazine derivs. of formula (I) and their acid-addn. and quat. salts are new. R1 is H or phenyl opt. subtd. by 1-4C alkyl, halogen, 1-4C alkoxy and/or NO2; R2 is 1-4C alkyl, 5-7C cycloalkyl, naphthyl, or phenyl opt. substd. as above; R3 is H, 1-4C alkyl or acyl; R4 is H or 1-...

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Hauptverfasser: SIMAY A, ECSERY-PUSKAS M, VIRAGH S, LITERATY-NAGY P, JUHASZ-NAGY S, SZEGI J, KISS-AJZERT I, HETYEY-PAPR M, TAKACZ K
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Sprache:eng
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Zusammenfassung:5,6-Dihydro-4H, 1,2,4-oxadiazine derivs. of formula (I) and their acid-addn. and quat. salts are new. R1 is H or phenyl opt. subtd. by 1-4C alkyl, halogen, 1-4C alkoxy and/or NO2; R2 is 1-4C alkyl, 5-7C cycloalkyl, naphthyl, or phenyl opt. substd. as above; R3 is H, 1-4C alkyl or acyl; R4 is H or 1-4C alkyl and R5 is 5-7C cycloalkyl, 1-6C alkyl, or phenyl (1-4C alkyl) in which the phenyl gp. is opt. substd. by 1-4C alkoxy, halogen or NO2, or R4+R5 is -CH2CH2-Ar-CH2-, where Ar is 4,5-di-R6-1,2-phenylene and R6 is H or 1-4C alkoxy; m and n are 0-2. Intermediates obtd. in the prepn. of (I) are also new. 7 Cpds. (I) are specifically claimed including 3-phenyl-6- 3-phenyl-6-cyclohexylaminomethyl-5,6-dihydro-4H-1,2, 4-oxadiazine. (I) are powerful peripheral vasodilators and hypotensives, giving increased coronary blood flow, having milk antiinflammatory and diuretic activity, and having potent antiarrhythmic activity.