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US 7,247,729 B2Granted
Method for producing pipecolamide derivative
AssigneeMercian Corporation
InventorsToshio Tsuchida, Katsura Kaneko, Naoki Matsumoto
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Abstract
A method of manufacturing a pipecolamide derivative, characterized in that pipecolic acid or an acid salt thereof is reacted with an amine in an inert solvent in the presence of a condensing agent such as dicyclohexylcarbodiimide, 1-ethyl-2-(2-dimethylaminopropyl)carbodiimide, methanesulfonyl chloride or phosphoryl chloride. Pipecolamide derivatives, particularly in optically active forms thereof can be efficiently and economically manufactured without harmful gas by-products.
Claims12
A method of manufacturing a topical anesthetic intermediate comprising reacting
- a) free pipecolic acid or an acid salt thereof
- b) with an aromatic amine
- c) in an inert solvent
- d) in the presence of a condensing agent, wherein the condensing agent is dicyclohexylcarbodiimide, 1-ethyl-3-(3′-dimethylaminopropyl)carbodiimide, methanesulfonyl chloride, or phosphoryl chloride,
- to produce a topical anesthetic intermediate selected from the group consisting of pipecolic acid-2,6-xylidide, pipecolic acid-2-toluidide, pipecolic acid-2,4,6-methidide, and pipecolic acid-2,4-xylidide.
2 more elements
Dependencies are inferred from the claim text.