Solid-phase synthesis of quinazolin-4(3H)-ones with three-point diversity
✍ Scribed by A.P. Kesarwani; G.K. Srivastava; S.K. Rastogi; B. Kundu
- Book ID
- 104251545
- Publisher
- Elsevier Science
- Year
- 2002
- Tongue
- French
- Weight
- 68 KB
- Volume
- 43
- Category
- Article
- ISSN
- 0040-4039
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✦ Synopsis
A versatile method for the solid-phase synthesis of differentially substituted quinazolin-4(3H)-ones has been developed using immobilized arylguanidines. The latter were obtained by treating the amino group of polymer-linked anthranilamide with isothiocyanates followed by coupling with secondary amines in the presence of DIC. Finally a cyclative cleavage strategy was applied to give the desired compounds in high yields and purities.
📜 SIMILAR VOLUMES
A solid-phase traceless synthesis of quinazolin-4-ones is described. An aldehyde functionalized resin was reductively aminated with primary amines, and the resin-bound secondary amine acylated with o-nitro-benzoic acids. The nitro group was reduced with tin(II) chloride, and the aniline acylated wit
## Abstract An approach for the solid‐phase synthesis of 4,8‐disubstituted‐8,9‐dihydropyrazino[2,3‐__g__]quinazolin‐7(6__H__)‐ones from 4‐chloro‐7‐fluoro‐6‐nitroquinazoline scaffold is described. A chemoselective reaction of resin‐bound arylamines (**3**) with 4‐chloro‐7‐fluoro‐6‐nitroquinazoline (