PRODUCTION OF NAPHTHAMIDE DERIVATIVE

PURPOSE: To obtain a naphthamide derivative useful as an antiallergic agent, etc., on an industrial scale in high yield by reacting a dihydroxynaphthoic acid derivative with an acyl compound and reacting the resultant compound with an (aminoethyl)-benzhydrylpiperidine. CONSTITUTION: The objective na...

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Bibliographic Details
Main Authors IKAWA HIROSHI, NISHIMURA MASAHITO
Format Patent
LanguageEnglish
Published 17.12.1996
Edition6
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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Summary:PURPOSE: To obtain a naphthamide derivative useful as an antiallergic agent, etc., on an industrial scale in high yield by reacting a dihydroxynaphthoic acid derivative with an acyl compound and reacting the resultant compound with an (aminoethyl)-benzhydrylpiperidine. CONSTITUTION: The objective naphthamide derivative of formula III is produced by reacting (A) a 3,5-dihydronaphthoic acid derivative of formula I ((n) is 1-6) with (B) an acyl compound of formula R COX (R is a 1-5C alkyl; X is a halogen) to obtain (C) a mixed acid anhydride of formula II (R is H or R CO) and reacting the mixed acid anhydride compound of formula III with (D) 1-(2- aminoethyl)-4-benzhydrylpiperidine. For example, N-[2-[4-benzhydryloxy) piperidino]ethyl]-3-hydroxy-5-(3-pyridylmethoxy)-2-naphthamide can be produced by reacting 3-hydroxy-5-(3-pyridylmethoxy)-2-naphthoic acid with pivaloyl chloride.
Bibliography:Application Number: JP19950160162