High Throughput Synthesis of Extended Pyrazolo[3,4-d]dihydropyrimidines

Autor: Alexander Shivanyuk, Dmitry S. Granat, Andrey S. Plaskon, Sergey V. Ryabukhin, Andrey A. Tolmachev, Yulian M. Volovenko
Rok vydání: 2012
Předmět:
Zdroj: ACS Combinatorial Science. 14:465-470
ISSN: 2156-8944
2156-8952
DOI: 10.1021/co300063x
Popis: Thirteen 5-hetarylaminopyrazoles were synthesized in 62-93% yield through the arylation of 1-isopropyl- and 1-phenyl-5-aminopyrazoles with electrophilic hetarylhalides under optimized conditions. Condensation of 5-hetarylaminopyrazoles with carbonyl compounds facilitated by AcOH or Me(3)SiCl furnished 23 pyrazolo[3,4-d]dihydropyrimidines in 69-86% yield. The target compounds were isolated through simple crystallization. The scope and limitation of the method are discussed.
Databáze: OpenAIRE