反应条件
1.1: p-toluenesulfonylazide; Et3N / acetonitrile / 0 - 20 °C
2.1: Rh2(OAc)4 / tetrahydrofuran; H2O / Heating
3.1: i-Pr2NEt / tetrahydrofuran / 0 °C
4.1: hydrogen / Pd(OH)2 on carbon / ethanol / 760 Torr
5.1: oxalyl chloride; DMF / CH2Cl2 / 0 - 20 °C
5.2: Bu4NBH4 / CH2Cl2 / -78 °C
6.1: 84 percent / CBr4; Ph3P / CH2Cl2 / 0 - 20 °C
View Scheme
参考文献
TAISHO PHARMACEUTICAL CO., LTD.; AMADA, Hideaki; MATSUDA, Daisuke; BOHNO, Ayako
Patent: WO2011/34215 A1, 2011 ;
WO 2011/034215 A1