Introduction and application of  CAS No. 315-30-0 | Allopurinol

Synonyms:4-HYDROXYPYRAZOLE[3,4-D]PYRIMIDINE;

4-HYDROXYPYRAZOLEO[3,4-D]PYRIMIDINE;

4-HYDROXYPYRAZOLO[3,4-D]PYRIMIDINE;

4’-hydroxypyrazolol(3,4-d)pyrimidine;

4-d)pyrimidin-4-one,1,5-dihydro-4h-pyrazolo

Specification:

preparation:

1) Put triethyl orthoformate, morpholine, acetonitrile, and cyanoacetamide into the reaction vessel in order and stir, heat the steam to reflux, and reflux for 4 hours. The initial reflux temperature will be 117°C, and the final reflux temperature will be 82°C. , the mixture obtained after the reflux is completed is cooled to 25-35°C, and then washed and vacuum dried sequentially to obtain the condensate;

2) Put the purified water, the condensate obtained in step 1), and hydrazine hydrate into the reaction vessel in order, stir, quickly heat to 90-100°C, and keep the temperature above 90°C for 20 minutes, and then cool the mixture to 60 ℃, then add dilute sulfuric acid and ice to perform hydrolysis and acidification reaction; collect the crystal hydrate after the acidification reaction reaches 5 ℃, and finally wash and vacuum dry the crystal hydrate to obtain the hemisulfate of 3-amino-4-pyrazole carboxamide;

3) Add the hemisulfate of 3-amino-4-pyrazole carboxamide to formamide, stir and heat to 140-150°C, and keep the reaction for 5 hours. After the reaction is completed, cool the reactant to 25-35°C and wash. Obtain crude allopurinol;

4) Crude allopurinol and activated carbon are added to concentrated hydrochloric acid for decolorization. The decolorized product is added to 25°C sodium hydroxide solution for recrystallization. Finally, it is washed and vacuum dried to obtain the allopurinol product.

Introduction:

Allopurinol is a white or off-white crystalline powder, almost odorless. Allopurinol is mainly used in the inter-attack and chronic stages of gout. It is suitable for those who produce excessive uric acid, are allergic to or ineffective with uricosuric drugs, and who are not suitable for using uricosuric drugs. The drug is used in patients with primary and secondary gout to control hyperuricemia. It can also be used in combination with uricosuric drugs to enhance the efficacy. It is especially suitable for patients with severe tophi and good renal function.

Indications:

1. Spontaneous and secondary hyperuricemia, especially hyperuricemia caused by excessive production of uric acid.

2. Recurrent or chronic gout;

3. Uric acid kidney stones and/or uric acid nephropathy;

4. Hyperuricemia with renal insufficiency.

Pharmacological effects and mechanism of action:

Allopurinol and its metabolite oxypurinol inhibit the activity of xanthine oxidase (the latter can convert hypoxanthine into xanthine, and then xanthine into uric acid), thereby reducing the production of uric acid, which is found in blood and urine. The uric acid content is reduced to a level below solubility, thus preventing the deposition of uric acid stones and helping to redissolve gout nodules and uric acid crystals.

Purpose:

Anti-gout medicine. It is suitable for various diseases with primary or secondary increase in serum uric acid, such as gout, acute or chronic leukemia, etc., and is used as an inhibitor of xanthine oxidase and pyridine synthesis.

Package and transportation :

Package: 10g,25g,50g,100g,250g

Transportation: by courier/ by air/ by sea