2-(5-bromopyrimidin-2-yl)ethanamine synthesis

Yield:914394-80-2 80%

Reaction Conditions:

Stage #1: tert-butyl [2-(5-bromopyrimidin-2-yl)ethyl]carbamatewith trifluoroacetic acid in dichloromethane at 20;
Stage #2: with sodium hydrogencarbonate in dichloromethane;water;

Steps:

Synthesis ofΗ-f2-(5-bromopyrimidin-2-yl)ethyll-2-(trifluoromethyl)benzamide (Compound 1)To a clear pale yellow mixture of the tert-butyl [2-(5-bromopyrimidin-2- yl)ethyl]carbamate (0.22g, 0.7mmol) in dichloromethane (2ml) was added trifiuoroacetic acid (10 equivs) and the mixture was left to stir at room temperature for 7 hrs and left to stand overnight. Saturated sodium bicarbonate solution was added until the effervescence stopped (to give a basic medium). The organic phase was collected, dried over MgSO4, and evaporated in vacuo after filtration, to yield to 0.12g of 2-(5-bromopyrimidin-2-yl)ethanamine (80%) which is used directly without purification.

References:

WO2006/117356,2006,A1 Location in patent:Page/Page column 30