2-Bromo-5-morpholinobenzonitrile synthesis
- Product Name:2-Bromo-5-morpholinobenzonitrile
- CAS Number:1129540-64-2
- Molecular formula:C11H11BrN2O
- Molecular Weight:267.12
Yield:1129540-64-2 30%
Reaction Conditions:
with potassium carbonate in dimethyl sulfoxide at 100; for 48 h;
Steps:
2-bromo-5-(4-morpholinyl)-benzonitrile (Intermediate 10)(Intermediate 10)A mixture of 2-bromo-5-fluorobenzonitrile (10 g, 50 mmol), morpholine (4.37 mL, 50 mmol), and potassium carbonate (6.91 g, 50 mmol), in DMSO (100 mL) was stirred at 100 °C for 48 h. The reaction mixture was poured into water (200 mL) and was stirred for 1 h. The precipitate was filtered off and purified by column chromatography on silica gel (eluent gradient from 50/50 to 100/0 DCM/heptane). The desired fractions were collected and evaporated, yielding 4.1 g (30 %) of Intermediate 10, after drying overnight under vacuum at 50 °C.
References:
WO2012/113850,2012,A2 Location in patent:Page/Page column 37
