Solid-phase synthesis of 2-aminoquinazolinone derivatives with two- and three-point diversity.
A versatile solid-phase method for the synthesis of various substituted 2-amino-4(3H)-quinazolinones with two- and three-point diversity is described. The synthesis commenced with the generation of polymer-bound S-methylisothiourea followed by N-acylation with different substituted o-nitrobenzoic acid. Finally, reduction of the nitro group triggered intramolecular cyclization via formation of guanidine to afford 2-amino-4(3H)-quinazolinone and its derivatives in high yields and purities.
Kundu
Bijoy
B
Medicinal Chemistry Division, Central Drug Research Institute, Lucknow, India. bijoy_kundu@yahoo.com
Partani
Pankaj
P
Duggineni
Srinivas
S
Sawant
Devesh
D