Basically substituted 4(3h)-quinazolinone derivatives

Abstract

Abstract THE PRESENT INVENTION RELATES TO PHARMACEUTICALLY ACTIVE BASICALLY SUBSTITUTED 4(3H)-QUINAZOLINONE DERIVATIVES POSSESSING ANTICONVULSANT AND SEDATIVE PROPERTIES AND USEFUL AS INTERMEDIATES IN THE MANUFACTURE OF CORONARY 2-R1,3-(R-CH2-CH(-OH)-CH2-),4-(O=),(R2)N-3,4-DIHYDRO- QUINAZOLINE OR THE CORRESPONDING EPOXY COMPOUND WITH A SECONDARY AMINE HAVING THE GENERAL FORMULA RH. QUINAZOLINE 2-R1,4-(O=),3-(HAL-CH2-CH(-OH)-CH2-),(R2)N-3,4-DIHYDRO- OR BY (C) CONDENSING A 4(3H)-QUINAZOLINONE WHICH IS SUBSTITUTED IN THE 3-POSITION BY A Y-HALOGENO-B-HYDROXYPROPYL RADICAL AND HAS THE FORMULA H2N-CH2-CH(OH)CH2-R WITH A Y-AMINO-B-HYDROXYPROPYLAMINE HAVING THE FORMULA 2-R1,4-(O=),(R2)N-4H-3,1-BENZOKAZINE OR BY (B) CONDENSING A 4H-3,1-BENZOXAZINE-4-ONE HAVING THE FORMULA HAL-CH2-CH(OH)CH2-R WITH A Y-HALOGENO-B-HYDROXYPROPYLAMINE HAVING THE FORMULA 2-R1,4-(O=),(R2)N-3,4-DIHYDROQUINAZOLINE DILATORS AND HAVING THE STRUCTURAL FORMULA WHEREIN R STANDS FOR A RADICAL SELECTED FROM THE GROUP CONSISTING OF SECONDARY ALIPHATIC, CYCLOALIPHATIC OR ARALIPHATIC AMINES HAVING 2-10 CARBON ATOMS AND 5-, 6- OR 7-MEMBERED HETEROCYCLIC NITROGEN BASES WHICH CONTAIN IN ADDITION TO THE NITROGEN ATOM A CORRESPONDING NUMBER OF METHYLENE GROUPS, AS WELL AS OPTIONALLY AN ADDITIONAL NITROGEN ATOM, AN O OR AN S ATOM, SAID RADICAL BEING BOUNS VIA A NITROGEN ATOM; R1 STANDS FOR HYDROGEN, AN ALKYL RADICAL HAVING FROM 1 TO 4 CARBON ATOMS, A PYRIDYL RADICAL, A BENZYL OR A PHENYL RADICAL, THE TWO LATTER BEING OPTIONALLY SUBSTITUTED BY LOWER ALKYL, LOWER ALKOXY GROUPS OR HALOGEN; R2 REPRESENTS HYDROGEN, NITRO, AMINO, TRIFLUOROMETHYL OR LOWER ALKOXY GROUPS HAVING FROM 1 TO 4 CARBON ATOMS, AND N MEANS AN INTEGER FROM 1 TO 4; AND TO THE PRODUCTION OF SUCH DERIVATIVES BY (A) REACTING A 4(3H)-QUINAZOLINONE HAVING THE FORMULA

Inventors

• 👤 R Beyerle
• 👤 A Stachel
• 👤 I Stachel

Bibliographic Details