Imidazo[1,2-a]pyrimidin-7-amine (9CI) synthesis
- Product Name:Imidazo[1,2-a]pyrimidin-7-amine (9CI)
- CAS Number:462651-80-5
- Molecular formula:C6H6N4
- Molecular Weight:134.14
Yield:462651-80-5 60%
Reaction Conditions:
with sodium hydrogencarbonate in ethanol;water at 70;
Steps:
199a Example 199a Imidazo[1,2-a]pyrimidin-7-amine 199a
Example 199a
Imidazo[1,2-a]pyrimidin-7-amine 199a
To the solution of pyrimidine-2,4-diamine (3.0 g, 0.027 mol) in ethanol (90 mL) and aqueous NaHCO3 (2M, 20 mL) was added 2-chloroacetaldehyde (4.3 g, 0.055 mol).
The mixture was stirred at 70°C overnight. TLC showed the starting material disappeared.
The solvent was removed under reduced pressure and the residue was extracted with ethyl acetate (3 X 30 mL).
The combined organic layer was concentrated under reduced pressure and the residue was purified by silica-gel column chromatography eluting with 1:5 petroleum ether/ethyl acetate to afford 199a as a white solid (2.2 g, 60%). MS: [M+H]+ 135.1.
References:
EP2773638,2015,B1 Location in patent:Paragraph 0765; 0766
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