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2005
Fused pyrimidine derivatives
R 0515
Liquid-Phase Synthesis of Combinatorial Libraries Based on 7-TrifluoromethPyrazolo[1,5-a]pyrimidine Scaffold. — More than 2200 carboxam32- 152 yl-Substituted
ides of type (V), (VI), (IX), and (X) are prepared on a 50—100-mg scale using special
CombiSyn synthesizers. Key reactions include assembly of the pyrazolo[1,5-a]pyrimidine ring by condensation of 5-aminopyrazole derivatives with trifluoromethyl-β-diketones. Target carboxamides are obtained from the condensation products by conversion
into acid chlorides, treatment of the latter with amines, and for the appropriate cases,
selective reduction of the pyrimidine ring by NaBH4. — (DALINGER, I. L.;
VATSADSE, I. A.; SHEVELEV, S. A.; IVACHTCHENKO*, A. V.; J. Comb. Chem. 7
(2005) 2, 236-245; Chem. Div. Labs, Inc., San Diego, CA 92121, USA; Eng.) —
Klein
2005
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