Synthetic method of pharmaceutical intermediate pyrano [2, 3-d] [1, 3] thiazolo [3, 2-a] pyrimidine derivative

Abstract

The invention relates to the field of pharmaceutical chemical industry, and particularly discloses a synthetic method of a pharmaceutical intermediate pyrano [2, 3-d] [1, 3] thiazolo [3, 2-a] pyrimidine derivative, which comprises the following steps: in a catalytic system consisting of a basic ionic liquid catalyst and a mixed solvent, taking aldehyde, malononitrile and 7-hydroxy-2, 3-dihydro-5H-[1, 3] thiazolo [3, 2-a] pyrimidine-5-ketone as raw materials, and reacting at the temperature of 60-80 DEG C to obtain the pyrano [2, 3-d] [1, 3] thiazolo [3, 2-a] pyrimidine derivative. And reacting at the temperature of between 35 and 50 DEG C for 4 to 8 minutes, and preparing to obtain the pyrano [2, 3-d] [1, 3] thiazolo [3, 2-a] pyrimidine derivative medical intermediate. According to the synthesis method, through selection of a plurality of elements such as catalyst, reaction solvent and catalytic system regeneration, the target product can be obtained at high yield, and the synthesis method has good industrial large-scale use value in the technical field of medical intermediate synthesis.

Description

technical field [0001] The invention relates to a synthesis method of derivatives, in particular to a synthesis method of a pharmaceutical intermediate pyrano[2,3-d][1,3]thiazolo[3,2-a]pyrimidine derivatives, belonging to the field of medicine and chemical industry . Background technique [0002] Pyrimidine derivatives are a very important class of active substances in the fields of pesticides and biomedicine, and have broad-spectrum biological activities, such as insecticidal, bactericidal, herbicidal, antiviral, and anticancer. The thiazolopyrimidine compound containing two important active unit structures of thiazole and pyrimidine is an important analogue of purine, which has biological activities such as anti-virus and anti-tumor, and has a wide range of uses in the field of medicine. Thiazolo[3,2-a]pyrimidine derivatives, as the most studied class of nitrogen and sulfur heterocyclic compounds with various important biological activities among thiazolopyrimidine compou...

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Problems solved by technology

[0004] But above-mentioned synthesis method also has the following problems: 1, the used organic base catalyst can not be recycled, also produces a large amount of waste liquids while increasing production cost, causes the rise of environmental pollution and treatment difficulty; 2, is lost in the environment The removed organic base catalyst is not easy to be degraded by microorganisms; 3, the selectivity of the catalyst is not high, so that a large amount of by-products are left in the reaction solvent, causing the reaction solvent to be difficult to recycle and reuse; 4, because the catalyst and the reaction solvent cannot be recycled, The whole synthesis process cannot be produced continuously, but can only be produced intermittently

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