title: Microwave-assisted, divergent solution-phase synthesis of 1,3,6-trisubstituted pyrazolo[3,4-d]pyrimidines.
abstract: A concise and highly divergent synthetic route has been developed to rapidly access 1,3,6-trisubstituted pyrazolopyrimidines. The synthesis features a microwave assisted one-pot N1-alkylation/Suzuki-Miyaura reaction as the key step. The sequence of the synthetic scheme can be varied to selectively modify the N1, C3, or C6 position at a late synthetic stage, thereby providing a highly efficient approach to explore the structure-activity relationships of pyrazolopyrimidine derivatives. The scope of these reactions has also been explored.
authors.affiliation: Center for Integrative Chemical Biology and Drug Discovery, Division of Medicinal Chemistry and Natural Products, Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, 27599, United States.
authors.forename: Jing
authors.initials: J
authors.lastname: Liu
authors.forename: Xiaodong
authors.initials: X
authors.lastname: Wang
mesh_terms: D020650:Combinatorial Chemistry Techniques / Q000379:methods*; D055808:Drug Discovery; D008872:Microwaves; D015394:Molecular Structure; D011720:Pyrazoles / Q000138:chemical synthesis*; D011743:Pyrimidines / Q000138:chemical synthesis*; D054852:Small Molecule Libraries / Q000138:chemical synthesis
chemical_list: D011720:Pyrazoles; D011743:Pyrimidines; D054852:Small Molecule Libraries