发明名称 PROCESS FOR PRODUCING 1-TRIAZOLE-2-BUTANOL DERIVATIVES
摘要 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 an acid addition salt of 4-methylenepiperidine in a reaction solvent in the presence of a hydroxide of an alkali metal or an alkaline earth metal selected from the group consisting of lithium, sodium, calcium, and strontium, or a hydrate thereof.
申请公布号 EP2966071(B1) 申请公布日期 2017.01.25
申请号 EP20150179288 申请日期 2011.08.31
申请人 KAKEN PHARMACEUTICAL CO., LTD. 发明人 Mimura, Mitsuo;Watanabe, Masahito;Ishiyama, Nobuo;Yamada, Takuya
分类号 C07D401/06 主分类号 C07D401/06
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