Synthesizing method of adenine

Abstract

The invention discloses a synthesizing method of adenine represented by a formula (I). The method comprises steps that: (1) acetyl hypoxanthine represented by a formula (III) and excess phosphorus oxychloride are subject to a chlorination reaction under the catalyzing of N,N-dimethyl aniline; the reaction is sufficiently carried out, and then 6-chloropurine represented by a formula (II) is obtained after processing; (2) in an autoclave, ammonia gas is delivered to an aqueous solution of 6-chloropurine until saturated; the autoclave is sealed, and a temperature in the autoclave is increased to120 to 140 DEG C; a reaction is processed until the materials are completely reacted; the pH value of the reaction liquid is regulated to 7-8; the reaction liquid is cooled, an adenine crude product is precipitated; the adenine crude product is refined by using water, and is processed through active carbon decoloration, such that adenine represented by the formula (I) is obtained. The synthesizing method provided by the invention is advantaged in high production efficiency, high reaction yield, good product quality, low three-waste rate, and low production cost.

Description

technical field The invention relates to the technical field of preparation methods of adenine. Background technique Adenine, Chinese name: 6-aminopurine (i.e. compound I), is an important pharmaceutical raw material and intermediate. Its phosphate, commonly known as vitamin B4, is a component of nucleic acid and participates in the synthesis of genetic material. It can promote the proliferation of white blood cells and increase the number of white blood cells. It is used to prevent and treat leukopenia caused by various reasons, especially for leukopenia caused by tumor chemotherapy, and also for acute neutropenia. Adenine is also an essential raw material for the preparation of anti-hepatitis B drugs adefovir dipivoxil and tenofovir dipivoxil (or "tenofovir dipivoxil"), adenosine and plant growth hormone 6-benzyl adenine. The synthetic route reported in the literature has the following several at present: Route 1 (CN101125854): Route 2 (1, JP 2002155082, 2, WO2005...

AI Technical Summary

Problems solved by technology

In practice, people such as Guo Chun (Guo Chun etc., fine chemical industry, 31-33,15,1998) acetyl hypoxanthine is dissolved with 70 times of hot water, adjusts pH=8 with 50% sodium hydroxide and obtains, yet The production efficiency of this operation is too low and the production cost is high