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The preparation method of Akatinib

A kind of technology based on acatinib and pyrazine, which is applied in the field of preparation of acatinib, which can treat leukemia, can solve the problems of low total yield, many reaction steps, and difficult industrialization, and achieve simple, environmentally friendly and economical process , promote the use and development of

Active Publication Date: 2019-05-07
哈尔滨医大药业股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] It can be seen from this that the existing preparation scheme of acatinib has problems such as many reaction steps and low total yield, and is limited by many aspects such as cost, equipment and environmental protection, and is not easy to be industrialized

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  • The preparation method of Akatinib
  • The preparation method of Akatinib
  • The preparation method of Akatinib

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Embodiment Construction

[0026] The technical solutions involved in the present invention will be described in further non-limiting detail below in conjunction with preferred embodiments.

[0027] One embodiment of the present invention provides a preparation method of Acalabrutinib that can be used for the treatment of leukemia, comprising the following steps:

[0028] Step S1:

[0029] Add 3-chloro-2-formaldehyde pyrazine (II) (0.71g, 5mmol) and dioxane (20mL) into the pressure reactor, and feed ammonia gas (1.7g, 0.1mol) under stirring, then add 4-(Pyridin-2-yl-aminocarbonyl)phenylboronic acid (III) (2.42 g, 10 mmol), rhodium acetylacetonate dicarbonyl (0.26 g, 1 mmol) and water 4 mL. Seal the reactor, gradually raise the temperature to 80-90 degrees, react for 16-18 hours, TLC detection, the reaction is complete. Concentrate under reduced pressure, dissolve the residue with dichloromethane, wash with saturated sodium bicarbonate and water successively, and dry over anhydrous sodium sulfate. Con...

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Abstract

The invention discloses a preparation method of a new drug acalabrutinib applicable to treatment of leukemia. The preparation method comprises the steps of condensation, acylation, cyclization, amination and other reactions by using 3-chloro-2-formylpyrazine as the raw material, thereby obtaining the acalabrutinib. The preparation method of acalabrutinib has the advantages of accessible raw materials, simple technique and the like, is economical and environment-friendly, and is suitable for large-scale industrial production.

Description

technical field [0001] The invention belongs to the technical field of organic synthesis route design and preparation of raw materials and intermediates, and particularly relates to a preparation method of Acalabrutinib, which can treat leukemia. Background technique [0002] Acalabrutinib (ACP-196) is a highly selective and irreversible second-generation BTK inhibitor developed by Acerta Pharma, a subsidiary of AstraZeneca. The drug can play its role by permanently binding BTK. Inhibits cancer cell growth signaling by blocking BTK until it promotes cancer cell death. In September 2015, the U.S. Food and Drug Administration (FDA) granted the drug the orphan drug qualification for the treatment of mantle cell lymphoma; in March 2016, the European Medicines Agency (EMA) granted the drug the treatment of chronic lymphocytic leukemia / small lymphocytic lymphoma, Orphan drug status for three indications including mantle cell lymphoma and lymphoplasmacytoid lymphoma. Since Acalab...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D487/04A61P35/02
CPCC07D487/04
Inventor 许学农
Owner 哈尔滨医大药业股份有限公司