BENZAZATHIINE DERIVATIVE AND ITS PREPARATION

NEW MATERIAL:A compound of formula 1 [R is H, formula 11 (R is alkyl, cylcoalkyl, phenylalkyl); R is H, benzyl, carbobenzoxyl] or its acid adduct. EXAMPLE:5-[3-(3, 4-Dimethoxyphenethylamino)-2-hydroxypropoxy]3, 4-dihydro-1,2- benzazathiine2,2-dioxide. USE:It is expected to be used as a medicine for...

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Bibliographic Details
Main Author HORI MIKIO
Format Patent
LanguageEnglish
Published 17.09.1984
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:NEW MATERIAL:A compound of formula 1 [R is H, formula 11 (R is alkyl, cylcoalkyl, phenylalkyl); R is H, benzyl, carbobenzoxyl] or its acid adduct. EXAMPLE:5-[3-(3, 4-Dimethoxyphenethylamino)-2-hydroxypropoxy]3, 4-dihydro-1,2- benzazathiine2,2-dioxide. USE:It is expected to be used as a medicine for circulation system, because of its very strong beta1-receptor inhibiting action. PREPARATION:Bromination of 2-methyl-3-nitroanisol of formula 2 is followed by reaction with methanesulfonic acid ester to give a compound of formula 4. The product is converted into a free acid, then the free acid is subjected to reduction and cyclization to give a compound of formula 9 (compound of formula I other than those where R is H and R is H). The compound is allowed to react with epihalohydrin in the presence of a base to form a compound of formula 10, which is made to react with an amine to give a compound of formula 1 where R is formula 11.
Bibliography:Application Number: JP19830037541