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(4-Methyl-1-(tetrahydro-2H-pyran-2-yl)-1H-benzo[d]iMidazol-5-yl)MethanaMine synthesis
- Product Name:(4-Methyl-1-(tetrahydro-2H-pyran-2-yl)-1H-benzo[d]iMidazol-5-yl)MethanaMine
- CAS Number:1425933-32-9
- Molecular formula:C14H19N3O
- Molecular Weight:245.32
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Yield: 70%
Reaction Conditions:
with ammonia;hydrogen in methanol at 25; for 2 h;
Steps:
18.6
step 6: A mixture of 162 (9.8 g, 52.5 mmol), MeOH (NH3 in MeOH) and Raney-Ni (> 15 eq) was stirred under hydrogen at 25 °C for 2 h. The mixture was filtered and concentrated in vacuo. The crude product was purified by Si02 chromatography eluting with a MeOH/DCM gradient (0%> to 10%> MeOH) to afford 7.0 g (70%)) of (4-methyl-l-tetrahydropyran-2-yl-benzimidazol-5-yl)methanamine (164) as yellowish oil: LC/MS: m/z =246 [M+l]+.
References:
F. HOFFMANN-LA ROCHE AG;ALIAGAS-MARTIN, Ignacio;CRAWFORD, James;LEE, Wendy;MATHIEU, Simon;RUDOLPH, Joachim WO2013/26914, 2013, A1 Location in patent:Page/Page column 143
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