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  • Title: An efficient and regiospecific strategy to N7-substituted purines and its application to a library of trisubstituted purines.
    Author: Liu J, Dang Q, Wei Z, Shi F, Bai X.
    Journal: J Comb Chem; 2006; 8(3):410-6. PubMed ID: 16677011.
    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.
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