Preparation of a fully substituted purine library.
A library of tetra-substituted purine analogues was readily prepared via parallel synthesis. This strategy relies on a key cyclization of a 4,5-diaminopyrimidine with either a carboxylic acid or its derivative to construct the 2,8,9-trisubstituted 6-chloropurine core. Further elaborations of this core allow the introduction of other diversity points. This methodology is demonstrated through the preparation of a 135-membered library of tetra-substituted purines in good yields and high purity.
Yang
Jianxin
J
The Center for Combinatorial Chemistry and Drug Discovery, Jilin University, 75 Jinlai Street, Changchun, Jilin 130012, PR China.
Dang
Qun
Q
Liu
Jinglin
J
Wei
Zhonglin
Z
Wu
Jinchang
J
Bai
Xu
X
D000818:Animals; D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D020650:Combinatorial Chemistry Techniques; D003500:Cyclization; D015195:Drug Design; D004353:Drug Evaluation, Preclinical; D015394:Molecular Structure; D011687:Purines / Q000138:chemical synthesis* / Q000494:pharmacology; D011743:Pyrimidines / Q000737:chemistry
D000998:Antiviral Agents; D011687:Purines; D011743:Pyrimidines