A kind of preparation method of pazopanib and its intermediate

A system and compound technology, applied in the field of medicine and chemical industry, can solve the problems of harsh reaction conditions, high industrialization cost, complicated purification operation, etc., and achieve the effects of mild reaction conditions, reducing the generation of by-products, and simplifying the purification operation.
CN107721989BActive Publication Date: 2019-06-14苏州东南药业股份有限公司
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
苏州东南药业股份有限公司
Publication Date
2019-06-14

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Abstract

The invention discloses a preparation method and an intermediate of Pazopanib. The preparation method comprises the steps of carrying out two-step condensation reaction on 2,4-dichloro-5-nitropyrimidine so as to obtain a compound of a formula 5 (shown in the description), and carrying out reduction on the compound of the formula 5, so as to obtain Pazopanib. The preparation method has the beneficial effects that the yield of Pazopanib is increased, reaction conditions are mild, column chromatography purification is not required, and the preparation method is applicable to industrial production.
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Description

technical field

[0001] The invention belongs to the field of medicine and chemical industry, and in particular relates to a preparation method of pazopanib and an intermediate thereof. Background technique

[0002] Pazopanib (Pazopanib) is a new oral angiogenesis inhibitor developed by GlaxoSmithKline that can interfere with the formation of new blood vessels required for the survival and growth of stubborn tumors, targeting the vascular endothelial growth factor receptor ( VEGFR), which acts by inhibiting the formation of new blood vessels to the tumor blood supply. In vitro, pazopanib inhibited ligand-induced autophosphorylation of VEGFR-2, Kit, and PDGFR-receptors, and in vivo, pazopanib inhibited VEGF-induced phosphorylation of VEGFR-2 in mouse lung, Angiogenesis in a mouse model, and xenograft growth of several human tumors in mice. It is indicated for the treatment of advanced renal cell carcinoma (a type of kidney cancer in which cancer cells are found in the kidney...

Claims

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