High throughput synthesis of extended pyrazolo[3,4-d]dihydropyrimidines.

Autor: Ryabukhin SV; The Institute of High Technologies, Kyiv National Taras Shevchenko University, Ukraine. s.v.ryabukhin@gmail.com, Granat DS, Plaskon AS, Shivanyuk AN, Tolmachev AA, Volovenko YM
Jazyk: angličtina
Zdroj: ACS combinatorial science [ACS Comb Sci] 2012 Aug 13; Vol. 14 (8), pp. 465-70. Date of Electronic Publication: 2012 Jul 20.
DOI: 10.1021/co300063x
Abstrakt: 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: MEDLINE