Zeghida Walid, Debray Julien, Chierici Sabine, Dumy Pascal, Demeunynck Martine
Département Chimie Moléculaire, UMR 5250, Université Joseph Fourier, BP 53, 38041 Grenoble cedex 9, France.
J Org Chem. 2008 Mar 21;73(6):2473-5. doi: 10.1021/jo7026883. Epub 2008 Feb 22.
A novel and simple method of preparation of 2-alkylaminoquinazolin-4-ones with fused heteroaromatic rings from easily accessible (hetero)aromatic amines is described. The method is very efficient, and the 2-alkylaminoquinazolinone derivatives are obtained in three steps without chromatographic purification. The key step is the ring closure of the N-protected guanidine intermediates by intramolecular Friedel-Craft's type substitution.
描述了一种从易于获得的（杂）芳族胺制备具有稠合杂芳环的2-烷基氨基喹唑啉-4-酮的新颖且简单的方法。该方法非常有效，无需色谱纯化即可通过三步获得2-烷基氨基喹唑啉酮衍生物。关键步骤是通过分子内傅克型取代使N-保护的胍中间体闭环。
