83768-03-0Relevant articles and documents
Substituted pyrimidin-2-ones and the salts thereof
-
, (2008/06/13)
Compounds of the general formula: STR1 (wherein X represents a halogen atom or a trifluoromethyl group; R1 and R2 independently represent a hydrogen atom or a lower alkyl group; Z is --O--, --S--, --SO--, --SO2 -- or the group --NR4 -- wherein R4 is as defined for R hereinafter or represents the group COR5 in which R5 represents a hydrogen atom or an optionally substituted aryl, heterocyclic, aralkyl, lower alkyl or lower alkoxy group; R represents a C6-10 carbocyclic aromatic group or a heterocyclic group containing a 5-9 membered unsaturated or aromatic heterocyclic ring which ring contains one or more heteroatoms selected from O, N and S and optionally carries a fused ring which carbocyclic or heterocyclic group may carry one or more C1-4 alkyl or phenyl groups, said groups being optionally substituted; or, where Z represents the group >NR4, the group --ZR may represent a heterocyclic ring optionally carrying a fused ring and/or optionally substituted as defined for R; and R3 represents a hydrogen atom or a lower alkyl, lower alkenyl, lower alkynyl, lower alkanoyl, lower alkenoyl, C7-16 aralkyl or C6-10 arly group or a 5-9 membered unsaturated or aromatic heterocyclic ring); and, where acid or basic groups are present, the salts thereof; are useful in combating abnormal cell proliferation. The compounds of the invention are prepared by inter alia alkylation, ring closure and oxidation.
α-Haloalkyl Ethers in Alkylations of 2-Pyrimidinones
Benneche, Tore,Undheim, Kjell
, p. 345 - 350 (2007/10/02)
The ambident 5-halopyrimidin-2-one anion with potassium as counterion in DMF is preferentially O-alkylated using the relatively hard α-chloroalkyl ether electrophiles.As ammonium salts in dichloromethane or by the use of KF-alumina in DME the preference is for N-alkylation.TMS ethers of the pyrimidinones are exclusively N-alkylated.
