Synthesis method of 4-chloropyrrolopyrimidine compound

A technology of chloropyrrolopyrimidine and a synthesis method, which is applied in the field of synthesis of 4-chloropyrrolopyrimidine compounds, can solve the problems of long synthesis route, high toxicity of raw materials, environmental pollution and the like, and achieves short synthesis route, low toxicity of raw materials and pollution. light effect
CN111454261AInactive Publication Date: 2020-07-28南京普锐达医药科技有限公司
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
南京普锐达医药科技有限公司
Publication Date
2020-07-28
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention particularly relates to a synthetic method of a 4-chloropyrrolopyrimidine compound. The method comprises the following steps: step 1, mixing 4-hydroxypyrrolopyrimidine, phosphorus oxychloride and an organic alkali according to a weight ratio of 1: (5-10): (3-7), carrying out a chlorination reaction in a certain temperature range, carrying out reduced pressure concentration to removeredundant phosphorus oxychloride, quenching, extracting, drying, and concentrating to obtain 4-chloropyrrolopyrimidine; step 2, dissolving 4-chloropyrrolopyrimidine in ethanol, starting to dropwise add an ethanol solution of ammonia, carrying out a reaction at a constant temperature, and removing excess ethanol to obtain 4-aminopyrrolopyrimidine; step 3, dissolving 4-aminopyrrolopyrimidine in dichloromethane, adding iodo-succinimide in batches at the room temperature, filtering to remove solid insoluble substances, and completely evaporating the filtrate to obtain 4-amino-5-iodopyrrolopyrimidine; and step 4, dissolving 4-amino-5-iodopyrrolopyrimidine in DMF, adding cesium carbonate and methyl iodide, carrying out a reflux reaction for 12 h, cooling, filtering, and evaporating to obtain theproduct namely 4-amino-5-iodine-7-methylpyrrolopyrimidine.
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Description

technical field

[0001] The invention belongs to the technical field of synthesis of pharmaceutical intermediates, and in particular relates to a synthesis method of a 4-chloropyrrolopyrimidine compound. Background technique

[0002] In recent years, heterocyclic compounds have attracted extensive attention due to their wide application in medicinal chemistry research. Heterocyclic compounds are cyclic compounds containing at least two different elements as ring member atoms, the most common atoms including nitrogen, oxygen and sulfur. Heterocyclic compounds exist in abundance in nature, and are of great significance in our lives because they exist in various natural molecules such as hormones, antibiotics, and caffeine. Pyrimidine rings are heterocyclic aromatic compounds that widely exist in nature. Pyrimidines were recognized as an important building block of nucleic acids in the early days and are currently used in AIDS chemotherapy.

[0003] 4-Chloropyrrolopyrimidine,...

Claims

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