METHOD OF /2S,3S/-3-HYDROXY-2-/4-METHOXYPHENYL/-2,3-DIHYDRO-1, 5-BENZOTHIAZEPINE-4/5H/-ON PRODUCTION

METHOD OF /2S,3S/-3-HYDROXY-2-/4-METHOXYPHENYL/-2,3-DIHYDRO-1, 5-BENZOTHIAZEPINE-4/5H/-ON PRODUCTION

The solution concerns a method of production of (2S, 3S)-3-hydroxy-2-(4-methoxyphenyl)-2,3-dihydro-1,5-benzothiazepamine-4(5H)-one of formula I, an intermediate product of an important cardiovascular pharmaceutical diltiazem, which has an antihypertensive effect and acts as calcium antagonist. The c...

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Hauptverfasser: HAAS ZDENEK ,CS, BELUSA JINDRICH ,CS, TREFULKA MOJMIR ,CS, KAMINSKA ZDENA,CS, HRUSKOVA VERA RNDR.,CS, PICHA FRANTISEK RNDR.,CS, WOJNAR VLADIMIR ,CS, STUDENCIK ZDENEK RNDR.,CS
Format: Patent
Sprache:eng
Schlagworte:
CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
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Zusammenfassung:The solution concerns a method of production of (2S, 3S)-3-hydroxy-2-(4-methoxyphenyl)-2,3-dihydro-1,5-benzothiazepamine-4(5H)-one of formula I, an intermediate product of an important cardiovascular pharmaceutical diltiazem, which has an antihypertensive effect and acts as calcium antagonist. The complicated production method is simplified by using, as initial material, lysine salt of (2S, 3S)-3-(2-aminophenylthio)-2-hydroxy-3-(4-methoxyphenyl) propionic acid of formula II, obtained by optical resolution of racemic acid in the form of centrifuged and non-dried cake. All the L-lysine is returned back to the technological process.