Synthesis Of The Derivatives Of Quinazolinone

Quinazolinone class of nitrogen-containing heterocyclic compounds with good biomedicine activity, bactericidal, anti-inflammatory, analgesic, fungicidal, anti-spasm, anti-hypertensive, anti-diabetic, anti-cancer, etc. are showing goodbiological activity. The important natural alkaloids also contain Quinazolinone skeleton, for example, having antimalarial trona class, as febrifugine.Quinazolinone or synthesis of fine chemicals and pharmaceutical intermediates, such as by the quinazolinone through chlorination, ammoniation obtained4aminoquinoline azole is a basic skeleton of a series of drug. In addition the intermediate Quinazolinone also an important synthetic thymidylate synthase inhibition, constitute the basic skeleton of the nucleus.This research project is the synthesis of various quinazoline derivatives as a further synthesis of thymidylate synthase inhibition intermediates.1. Novel thymidylate synthase inhibitors of the intermediates were synthesized with m-nitrobenzaldehyde. With benzaldehyde as raw material, through ammonia water protection, nitration, hydrolysis, aldol reaction, finally to obtain the final product between nitro cinnamic aldehyde. And the corresponding nitrification and aldol condensation reaction were optimized, and increasing yield.2. Corresponding to aniline compounds as the raw material, an important intermediate of isatin derivatives7-isatin chloride,5-isatin chloride,7-methyl isatin,5-methyl isatin and5-bromide isatin synthesis. 3.By the corresponding7-isatin chloride,5-isatin chloride and5-bromide isatin as starting material,will be carried out with hydrazine isatin reduction.Thus were synthesized with corresponding indole-2-ketone compounds7-chloro-indole-2-ketone,5-chloro-indole-2-ketone and5-bromo-indole-2-ketone.