Synthesis of pyrazolo [3, 4-d]-4, 5-dihydropyrimidin-6-ones

SV Ryabukhin, DS Granat, AS Plaskon, A Shivanyuk…

Index: Ryabukhin, Sergey V.; Granat, Dmitry S.; Plaskon, Andrey S.; Shivanyuk, Alexander; Lukin, Oleg Tetrahedron Letters, 2014 , vol. 55, # 10 p. 1846 - 1847

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Citation Number: 2

Abstract

Abstract A small library of hitherto unprepared pyrazolo [3, 4-d]-4, 5-dihydropyrimidin-6-ones was synthesized on a preparative scale. The synthesis starts with a substituted 5- aminopyrazole that reacts with an isocyanate to give the corresponding urea. The latter undergoes a chlorotrimethylsilane-promoted [5+ 1] cyclocondensation with an aldehyde yielding the title pyrazolo [3, 4-d]-4, 5-dihydropyrimidin-6-one. Both synthetic steps are ...