The regioselective bromine-lithium exchange reaction of alkoxymethyldibromobenzene: A new strategy for the synthesis of tofogliflozin as a SGLT2 inhibitor for the treatment of diabetes

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• 作者：Masatoshi Murakata ; ^{murakatamst@chugai-pharm.co.jp} ; Takuma Ikeda ; Nobuaki Kimura ; Akira Kawase ; Masahiro Nagase ; Masahiro Kimura ; Kenji Maeda ; Akie Honma ; Hitoshi Shimizu
• 关键词：Bromine-lithium exchange reaction ; Regioselective ; Sequential metalation-functionalization ; Tofogliflozin
• 刊名：Tetrahedron
• 出版年：2017
• 出版时间：9 February 2017
• 年：2017
• 卷：73
• 期：6
• 页码：655-660
• 全文大小：531 K
• 卷排序：73

文摘

Highly regioselective bromine-lithium exchange reaction of dibromobenzene derivative was realized. Dibromide as a starting material was found to be a mediator that increased the selectivity. Tofogliflozin was synthesized via three-component coupling.