Allopurinol synthesis
- Product Name:Allopurinol
- CAS Number:315-30-0
- Molecular formula:C5H4N4O
- Molecular Weight:136.11
64-18-6
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315-30-0
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Yield:315-30-0 96%
Reaction Conditions:
Stage #1: 2-cyano-3-morpholinoacrylamidewith hydrazine hydrate in water at 90 - 100;
Stage #2: formic acid;formamide at 100 - 170;
Steps:
1.2; 2.2; 3-5 2. Preparation of 1H-pyrazolo[3,4-d]pyrimidin-4-ol:
2-cyano-3-morpholine acrylamide (65 g, 0.358 mol) was sequentially added to a 1000 ml three-necked flask.Hydrazine hydrate (19.2g, 0.38mol), 300g of water, and the temperature is raised to 90-100 °C for 0.5 to 1 hour. Additional formic acid (20 g, 0.37 mol), Formamide (200 g, 4.4 mol), the temperature is raised to 100-170 °C for 5-7 hours, and cooled to room temperature. filter, washing with a 1:10 volume ratio of ethanol solution, and recrystallized from water to obtain a white product of 42 g. Yield 96%,
References:
CN108822113,2018,A Location in patent:Paragraph 0024; 0027-0028; 0033; 0036; 0039; 0042
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315-30-0
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