Process for the preparation of substituted pyrimidines
AssigneeAmerican Cyanamid Company
InventorsOliver Meyer, Dieter Gutheil
Life of this patent
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Abstract
The invention relates to a process for the preparation of substituted pyrimidines of formula I, wherein R1, R2, R3, R4 and X are as defined in claim 1, which comprises reacting an amidine of formula II, or a salt thereof, with a 3,3-disubstituted vinylcarbonyl compound of formula III wherein L represent a halogen atom or a group of formula —X—R2, (a) in an inert solvent, in the presence of a base and a compound of formula IV H—X—R2 (IV) in the event that L represent a halogen atom, or (b) in an inert solvent and in the presence of a base, in the event that L represents a group of formula —X—R2.
Claims10
A process for the preparation of substituted pyrimidines of formula I,
- wherein
- R1 and R2 each independently represent an optionally substituted alkyl, cycloalkyl, phenyl or heteroaryl group,
- R3 and R4 each independently represent a hydrogen atom or an optionally substituted alkyl or phenyl group, and X represents O or S, which comprises reacting an amidine of formula II,
- or a salt thereof, wherein R1 has the meaning given for formula I, with a 3,3-disubstituted vinylcarbonyl compound of formula III
- wherein R3 and R4 have the meaning given, and L represent a halogen atom or a group of formula —X—R2,
- (a) in an inert solvent, in the presence of a base and a compound of formula IV
- H—X—R2 (IV)
- wherein X and R2 have the meaning given, in the event that L represent a halogen atom, or
- (b) in an inert solvent and in the presence of a base, in the event that L represents a group of formula —X—R2.
Dependencies are inferred from the claim text.