Synthetic process of 7‑bromo‑4‑chlorothieno[3,2‑d]pyrimidine

A synthesis process, a technology for chlorothiophene, applied in directions such as organic chemistry, can solve problems such as unfavorable large-scale application, low yield, affecting total yield, etc., and achieve the effects of increasing individual yields, increasing total yields, and reducing costs
CN105218560BActive Publication Date: 2017-09-29上海泰坦科技股份有限公司
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
上海泰坦科技股份有限公司
Publication Date
2017-09-29

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Abstract

The invention relates to a synthetic method of 7-bromo-4-chlorothieno [3,2-D] pyrimidine. The synthetic method comprises the following steps: adding 3-amino-2-methyl formate thiophene and formamide into ethylene glycol monomethyl ether, heating to 120-140 DEG C to reflux, then adding saturated salt water when a solvent is not reduced anymore, and filtering to obtain solid 4-hydroxyl thieno-pyrimidine; adding 4-hydroxyl thieno-pyrimidine, N-bromo-succinimide and sodium hexametahposphate into acetone, reacting at 5-30 DEG C, filtering, adding water into a filtrate, stirring, filtering, and collecting solids to obtain 4-hydroxyl-7-bromo-thieno-pyrimidine; and adding the 4-hydroxyl-7-bromo-thieno-pyrimidine into phosphorus oxychloride, heating to reflux, then pouring into ice water, stirring until solids are generated, filtering, and drying in the air to obtain 7-bromo-4-chlorothieno [3,2-D] pyrimidine. By use of the synthetic process, the total yield of the 7-bromo-4-chlorothieno [3,2-D] pyrimidine is improved, the cost is effectively reduced. The synthetic method of 7-bromo-4-chlorothieno [3,2-D] pyrimidine is suitable for industrial large-scale synthesis application.
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Description

technical field

[0001] The invention relates to a synthesis process of thienopyrimidine compounds, in particular to a synthesis process of 7-bromo-4-chlorothieno[3,2-D]pyrimidine. Background technique

[0002] Thienopyrimidine heterocyclic compounds have bactericidal, herbicidal, insecticidal and medicinal activities, and have broad application prospects, especially thienopyrimidines are a new type of anti-tumor drugs that inhibit SRC family protein kinases. The synthesis of an important intermediate 7-bromo-4-chlorothieno[3,2-D]pyrimidine (namely: 7-bromo-4-chlorothieno[3,2-D]pyrimidine, CAS No. : 31169-27-4), so it is of great significance and application value to study the synthetic method and process improvement of this intermediate. The structural formula of 7-bromo-4-chlorothieno[3,2-D]pyrimidine is shown below.

[0003]

[0004] CN102250111A (published date 2011.11.23) discloses a preparation method of 7-bromo-4-chlorothienopyrimidine, using 3-aminothiophene-2-ca...

Claims

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