5-halogeno-6-amino-nicotinic acid halides

US4895950A · kind A · utility

Assignee

• BAYER HEALTHCARE LLC · DE

Inventors

• Hans Lindel · Leverkusen, DE
• Werner Hallenbach · Nordhorn, DE

Key dates

• Filing date: Jul 7, 1988
• Grant date: Jan 23, 1990
• Expiry date: Jul 7, 2008

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D213/78
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

Novel 5-halogeno-6-amino-nicotinic acid halides of the formula ##STR1## in which R represents hydrogen or alkyl, PA0 R.sup.1 represents hydrogen, alkyl or acyl or PA0 R and R.sup.1, together with the nitrogen atom to which they are bonded, represent an optionally substituted heterocyclic radical, PA0 R.sup.2 represents halogen and PA0 Hal represents halogen, are prepared by halogenating the corresponding nicotinic acids. The Co Hal moiety is converted to CH.sub.3 by reaction with EQU R.sup.3 OMgCR.sup.4 (COOR.sup.3).sub.2 (IV) in which PA0 R.sup.3 represents C.sub.1-3 alkyl and PA0 R.sup.4 represents hydrogen or C.sub.1 -C.sub.2 -alkyl, and then hydrolyzing and decarboxylating the product.