Process for the preparation of substituted pyrimidines

US6281358A · kind A · utility

Assignee

• American Cyanamid Company · US

Inventors

• Oliver Meyer · Ingelheim am Rhein, DE
• Dieter Gutheil · Bretzenheim, DE

Key dates

• Filing date: Apr 12, 2000
• Grant date: Aug 28, 2001
• Expiry date: Apr 12, 2020

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D401/14
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

The invention relates to a process for the preparation of substituted pyrimidines of formula I, ##STR1## wherein PA1 R.sup.1, R.sup.2, R.sup.3, R.sup.4 and X are as defined in claim 1, which comprises reacting an amidine of formula II, ##STR2## or a salt thereof, with a 3,3-disubstituted vinylcarbonyl compound of formula III ##STR3## wherein L represent a halogen atom or a group of formula --X--R.sup.2, PA1 (a) in an inert solvent, in the presence of a base and a compound of formula IV EQU H--X--R.sup.2 (IV) in the event that L represent a halogen atom, or PA1 (b) in an inert solvent and in the presence of a base, in the event that L represents a group of formula --X--R.sup.2.