Kovalenko S. Synthesis, transformation, physico-chemical and biological properties of derivatives of quinazolone-4 and 4-aminoquinazoline.

Українська версія

Thesis for the degree of Doctor of Science (DSc)

State registration number

0500U000320

Applicant for

Specialization

  • 15.00.02 - Фармацевтична хімія та фармакогнозія

06-10-2000

Specialized Academic Board

Д 35.600.02

Danylo Halytsky Lviv National Medical University

Essay

The dissertation is dedicated to the elaboration of effective methods of synthesis of quinazolone-4 and 4-aminoquinazoline derivatives, determination of structure, invesstigation of calculations of quantun-mechanic indiced, physico-chemical properties, revealing of influence of structure features on chemical transformation, determination of connection between the conditions of alkalation and its direction, investigation of antioxydant activity and other kinds ol biological activity of the synthesized compounds. The preparative methods of synthesis of 2-R1-6-R2-8-R3-3-alkyl(benzyl-, oxyalkyl-, acylalkyl-)quinazoline-(3H)-4-ons, 2-R1-6-R2-8-R3-3- [b-brome-(R-amino-, ydrazine-, мercapto-)-ethyl]-quinazoline- (3H)-4-ons, 2-R2-6-R3-8-R4-(3H)-quinazolone-4-il-3 -a(b)-carbonic and 4-quinazolilaminoarylcarbonic acids and their derivatives, halogenides of 1-phenacul- 4-(4-sulfamidophenyl)aminoquinazolinium were worked out. The structure of the synthesised compounds wa s confirmed with the results of the element analysis, potentiometry, and by the methods of UV-, IR-, PMR-spectroscopy, mass-spectrophotometry and counter synthesis. The laboratory methods of synthesis, project of temporary pharmacopoeia article for the "Nitrocol" preparation, that is as an antioxydant and antiischaemic substance, were worked out.

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