反应条件
1.1: toluene-4-sulfonic acid / tetrahydrofuran / 60 °C / Inert atmosphere 2.1: lithium hexamethyldisilazane / tetrahydrofuran / 2.83 h / -25 - -15 °C / Inert atmosphere 2.2: 3.33 h / -20 - -15 °C / Inert atmosphere 3.1: acetonitrile / Inert atmosphere 4.1: 1,8-diazabicyclo[5.4.0]undec-7-ene / acetonitrile / 23 °C / Inert atmosphere 5.1: triethylamine / isopropanol acetate / 1.25 h / 0 - 10 °C / Inert atmosphere 6.1: sitagliptin transaminase CDX-017; triethanolamine; pyridoxal 5'-phosphate; N-isopropylamine hydrochloride / water; dimethyl sulfoxide / 11 h / 40 °C / pH 9.5 / Inert atmosphere 7.1: potassium carbonate / isopropanol acetate; water / 1.25 h / 0 °C / Inert atmosphere View Scheme
参考文献
MERCK SHARP and DOHME CORP.; MERCK SHARP and DOHME LIMITED; BAXTER, Carl, A.; CLEATOR, Edward; KRSKA, Shane, W.; SHEEN, Faye; STEWART, Gavin; STROTMAN, Neil; WALLACE, Debra, J.; WRIGHT, Timothy
Patent: WO2012/148553 A1, 2012 ;
WO 2012/148553 A1