1: With triphenylphosphine; diethylazodicarboxylate in toluene
T=60 - 115°C; 19 h;
2: With hydrogenchloride in water
3: With sodium hydroxide in water
T=5°C; pH=13;
1: 4-hydroxytetrahydro-4H-pyran With potassium tert-butylate in tetrahydrofuran
T=20°C; 0.333333 h;
2: 3-bromo-5-fluoro-pyridine in tetrahydrofuran
T=20°C;
参考文献
BOEHRINGER INGELHEIM INTERNATIONAL GMBH; STEURER, Steffen
Patent: WO2012/85127 A1, 2012 ;
Location in patent: Page/Page column 44 ;
WO 2012/085127 A1