The present invention provides compounds of formula (I) wherein A1, A2, R1, D1, D2, Y3 and X are as defined in the claims. The invention further relates to compositions which comprise these
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Page/Page column 117-118
(2012/05/31)
DIRECT INTRODUCTION OF ACYL AND ETHOXYCARBONYL GROUPS INTO PYRIMIDINE RING THROUGH THE TRIMETHYLSTANNYL DERIVATIVES
The reactions of acylformyl chlorides with 2- and 4-trimethylstannylpyrimidine derivatives proceeded more smoothly than those of acyl chlorides giving the corresponding 2- and 4-acylpyrimidines.Employing ethyl chloroglyoxylate instead of the acylating agent yielded the ethoxycarbonylpyrimidines.Similarly, the stepwise acylation and ethoxycarbonylation of bis(trimethylstannyl)pyrimidines provided pyrimidines having two different carbon functional groups.
It is shown that the use of benzene as the solvent in the preparation of 2- and 4-acetylpyrimidines from cyanopyrimidines via the Grignard reaction makes this reaction a practical method for the preparation of pyrimidinyl ketones.Preparatively convenient methods for the preparation of 4-acetylpyrimidine from 4-ethylpyrimidine through the α-oximino derivative and 5-acetylpyrimidine from 4,6-dichloro derivatives of pyrimidine are proposed.
Naumenko, I. I.,Mikhaleva, M. A.,Mamaev, V. P.
p. 710 - 714
(2007/10/02)
Studies on Pyrimidine Derivatives. XV. Homolytic Acylation and Amidation of Simply Substituted Pyrimidines
The reaction of 2,6-disubstituted pyrimidines with acyl radicals generated either from pyruvic acid-AgNO3-(NH4)2S2O8 ( method A ) or from aldehyde-FeSO4-t-BuOOH ( method B ) in aq.H2SO4, gave the corresponding 2,6-disubstituted 4-acylpyrimidines.However,