PROCESS FOR PRODUCING 1-TRIAZOLE-2-BUTANOL DERIVATIVES

PROCESS FOR PRODUCING 1-TRIAZOLE-2-BUTANOL DERIVATIVES

An object is to provide a process for producing the compound of formula 1 in higher yield by the ring-opening addition reaction of epoxytriazole with amine under mild conditions without using a large excess of 4-methylenepiperidine. The process for producing (2 R ,3 R )-2-(2,4-difluorophenyl)-3-(4-m...

Ausführliche Beschreibung

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Bibliographische Detailangaben
Hauptverfasser: ISHIYAMA, NOBUO, WATANABE, MASAHITO, YAMADA, TAKUYA, MIMURA, MITSUO
Format: Patent
Sprache:eng ; fre ; ger
Schlagworte:
CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
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Beschreibung
Zusammenfassung:An object is to provide a process for producing the compound of formula 1 in higher yield by the ring-opening addition reaction of epoxytriazole with amine under mild conditions without using a large excess of 4-methylenepiperidine. The process for producing (2 R ,3 R )-2-(2,4-difluorophenyl)-3-(4-methylenepiperidin-1-yl)-1-(1 H -1,2,4-triazol-1-yl)butan-2-ol or an acid addition salt thereof comprises reacting (2 R ,3 S )-2-(2,4-difluorophenyl)-3-methyl-2-[(1 H- 1,2,4-triazol-1-yl)methyl]oxirane with a hydroiodide salt of 4-methylenepiperidine in a reaction solvent in the presence of sodium hydroxide.