title: An efficient and regiospecific strategy to N7-substituted purines and its application to a library of trisubstituted purines.
abstract: A regiospecific strategy for the preparation of N(7)-substituted purines in an efficient manner was devised. This approach to 6,7,8-trisubstituted purines relies on the cyclization reactions of suitably substituted pyrimidines (1) with either a carboxylic acid or an aldehyde. The method development for the five-step synthetic strategy outlined here was completed using 5-amino-4,6-dichloropyrimidine (4) as the starting material. The utility of this methodology was demonstrated through the preparation of a 40-membered library of 6,7,8-trisubstituted purines (3) in good yields and high purity.
authors: The Center for Combinatorial Chemistry and Drug Discovery, Jilin University, Changchun, PR China.
authors: Jinglin
authors: J
authors: Liu
authors: Qun
authors: Q
authors: Dang
authors: Zhonglin
authors: Z
authors: Wei
authors: Fuqiang
authors: F
authors: Shi
authors: Xu
authors: X
authors: Bai