Heterogenous phase as a mean in combinatorial chemistry

Combinatorial chemistry is a rapid and inexpensive technique for the synthesis of hundreds of thous and s of organic compounds of potential medicinal activity. In the past few decades a large number of combinatorial libraries have been constructed, and significantly supplement the chemical diversity of the traditional collections of the potentially active medicinal compounds. Solid phase synthesis was used to enrich the combinatorial chemistry libraries, through the use of solid supports [resins] and their modified forms. Most of the new libraries of compounds appeared recently, were synthesized by the use of solid-phase. Solid-phase combinatorial chemistry [SPCC] is now considered as an outst and ing branch in pharmaceutical chemistry research and is used extensively as a tool for drug discovery within the context of high-throughput chemical synthesis. The best general pure libraries synthesized by the use of solid phase combinatorial chemistry [SPCC] may well be those of intermediate complexity that are free of artifact-causing nuisance compounds

Synthesis and reactions of 2-chloromethyl-6-iodo-3, 1-benzoxazin-4-one with amines

Certain quinazolinones were reported to exert antimicrobial activity[1]. Consequently, in continuation of our previous work on the reaction of 3,1-benzoxazin-4-ones with amines,[2-5], 2-chloromethyl-6- iodobenzoxazin-4-one was synthesized and allowed to react with amines hoping to obtain 4-quinazolinones for evaluation as antimicrobial agents. 5-Iodoanthranilic acid was chloroacetylated to give I which was cyclodehydrated to yield the corresponding 3,1-benzoxazin-4- one II Compound II was allowed to react with different aromatic amines to produce 3-aryl-2-chloromethyl-6-iodoquinazolin-4-ones IIIa-t. Structures of compounds III [Scheme 1] were confirmed by microanalytical and spectroscopic data [Table1 and 2]