2-Amino-4-chloro-7-((tetrahydro-2H-pyran-4-yl)methyl)-5H-pyrrolo[2,3-d]pyrimidin-6(7H)-one synthesis
- Product Name:2-Amino-4-chloro-7-((tetrahydro-2H-pyran-4-yl)methyl)-5H-pyrrolo[2,3-d]pyrimidin-6(7H)-one
- CAS Number:1196886-57-3
- Molecular formula:C12H15ClN4O2
- Molecular Weight:282.73
Yield:1196886-57-3 74%
Reaction Conditions:
with potassium tert-butylate in butan-1-ol; for 0.0833333 h;Reflux;
Steps:
III-55.1
To a solution of ethyl 2-(2-amino-4-chloro-6-((tetrahydro-2H-pyran-4- yl)methylamino)pyrimidin-5-yl)acetate (1 g, 3.05 mmol) in n-BuOH (100 mL) was added t- BuOK (30 mg, 0.27 mmol,). The solution was heated to reflux with stirring for 5 min. The resulting mixture was concentrated under vacuum. The residue was purified on a silica gel column with ethyl acetate/petroleum ether (1 :10), resulted in 640 mg (74%) of 2-amino-4- chloro-7-((tetrahydro-2H-pyran-4-yl)methyl)-5H-pyrrolo[2,3-d]pyrimidin-6(7H)-one as a yellow solid.
References:
WO2009/139834,2009,A1 Location in patent:Page/Page column 127
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