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ChemicalBook CAS DataBase List Allopurinol

Allopurinol synthesis

3synthesis methods
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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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