Synthesizing method for 4-amino-2-methyl-5-(brooethyl) pyrimidine hydrobromide

Abstract

The invention discloses a synthesizing method for 4-amino-2-methyl-5-(brooethyl) pyrimidine hydrobromide. The method comprises the following steps: acquiring formylated midbody sodium salt A by reacting 3-methoxypropionitrile with ethyl formate under the effect of sodium methylate; reacting the midbody sodium salt A with dimethyl sulfate, thereby acquiring a midbody B; condensing the midbody B with acetamidine hydrochloride, thereby acquiring a midbody C; and reacting the midbody C with hydrobromic acid, thereby acquiring a target product 4-amino-2-methyl-5-(brooethyl) pyrimidine hydrobromide I. According to the invention, the raw material source is wide and the cost is low; the synthesizing method is simple in production operation and has low requirement for processing equipment; the rigorous production conditions, such as, anhydrous condition, anaerobic condition and high-pressure hydrogenation, are not required; the reaction condition is mild; the method is easy for large-scale industrial production; the process is simple; the production period is short; the production efficiency is high; the production method is green and environmentally friendly and is suitable for large-scale industrial production.

Description

technical field [0001] The invention belongs to the field of organic chemistry, and in particular relates to a synthesis method of 4-amino-2-methyl-5-(bromomethyl)pyrimidine hydrobromide. Background technique [0002] 4-Amino-2-methyl-5-(bromomethyl)pyrimidine hydrobromide is an important pharmaceutical intermediate, which was first used in the total synthesis of vitamin B1, and can also be used as an important synthetic building block for other advanced drugs . Vitamin B1, also known as thiamine, was the first B vitamin to be identified. Thiamine-dependent enzyme acts as a cofactor for several enzymes involved in energy metabolism, which is important for the synthesis and production of neurotransmitters, substances used in the defense against oxidative stress reduction. Vitamin B1 mainly exists in the outer skin and germ of seeds, and the vitamin B1 currently used by people is the product of chemical synthesis. [0003] There are few reports on the synthesis of 4-amino-2...

AI Technical Summary

Problems solved by technology

[0008] 4-Amino-2-methyl-5-cyanopyrimidine is an important intermediate in the modern synthesis of vitamin B1. It is expensive and there are relatively few domestic manufacturers

The above-mentioned method 1 and method 2 have lengthy process routes, complex reactions, low yields and high costs, which limit their application in production

[0009] Method 3: U.S. Patent US2016122319 discloses a simple method of directly hydrogenating and reducing 4-amino-2-methyl-5-cyanopyrimidine under pressure, which requires 20 kg of pressure to achieve, which also limits its Application in actual production

[0010] It can be seen that the above process scheme has many reaction steps, cumbersome operation, difficult separation and purification, high cost, and does not meet environmental protection requirements. Therefore, it is urgent to develop a short synthetic route, simple operation, low cost, and green environmental protection. A new method of 2-methyl-5-(bromomethyl)pyrimidine hydrobromide

Images