4-(2-Chloro-5-methyl-5H-pyrrolo[3,2-d]pyrimidin-4-yl)morpholine synthesis

2synthesis methods

Product Name:4-(2-Chloro-5-methyl-5H-pyrrolo[3,2-d]pyrimidin-4-yl)morpholine
CAS Number:1375301-63-5
Molecular formula:C11H13ClN4O
Molecular Weight:252.7

110-91-8 Synthesis

110-91-8
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2,4-Dichloro-5-methyl-5H-pyrrolo[3,2-d]pyrimidine

129872-81-7
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$19.00/100mg

4-(2-Chloro-5-methyl-5H-pyrrolo[3,2-d]pyrimidin-4-yl)morpholine

1375301-63-5
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Yield:1375301-63-5 94%

Reaction Conditions:

with N-ethyl-N,N-diisopropylamine in N,N-dimethyl-formamide at 20; for 15 h;Inert atmosphere;

Steps:

101.2

Step 2: A mixture of 2,4-dichloro-5-methyl-5H-pyrrolo[3,2-d]pyrimidine (1.25 g,6.19 mmol), morpholine (1.08 mL, 12.37 mmol), and N,N-diisopropylethylamine (2.37 mL, 13.61 mmol) in N,N-dimethylformamide (36 mL) was stirred at RT under N₂ for 15h. The reaction mixture was diluted with 1 : 1 diethyl ether / ethyl acetate, and the organic layer was washed with 1 : 1 water / brine (3X) and brine (IX), dried over Na₂S0₄, filtered, and concentrated in vacuo. The crude product was purified by silica gel chromatography to give 1.47g (94.0%) of 4-(2-chloro-5-methyl-5H-pyrrolo[3,2-d]pyrimidin-4-yl)morpholine as a white solid. MS(ESI) m/z: 253.1/255.1 [M+l] ⁺.

References:

WO2012/82997,2012,A1 Location in patent:Page/Page column 86

2,4-DICHLORO-5H-PYRROLO[3,2-D]PYRIMIDINE

63200-54-4
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1375301-63-5
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References