Key intermediates for production of selective PI3K inhibitor

A technology of intermediates and inhibitors, applied in the fields of compounds containing elements of Group 3/13 of the periodic table, organic chemistry, chemical instruments and methods, etc., can solve the problems of large amount of butyllithium, low reaction temperature, and high equipment requirements , to achieve the effect of low cost, simplified reaction steps and broad market prospects
CN107793394AInactive Publication Date: 2018-03-13上海厚博生物科技有限公司
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
上海厚博生物科技有限公司
Publication Date
2018-03-13
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention discloses a series of key intermediates for production of a selective PI3K inhibitor. The structural formula of the key intermediates is shown in the description. The synthesis process of the key intermediates prevents complex processes, simplifies the reaction steps, utilizes easily available raw materials, utilizes mild reactions, realizes a low cost, is suitable for industrializedproduction and has a wide market prospect.
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Description

technical field

[0001] The invention relates to the field of pharmacy, in particular to a series of key intermediates for producing selective PI3K inhibitors. Background technique

[0002] 5-[2,6-bis(4-morpholinyl)-4-pyrimidinyl]-4-(trifluoromethyl)-2-pyridinylamine is a selective PI3K inhibitor developed by pharmaceutical giant Novartis, English The name is Buparlisib, code-named BKM120 or NVP-BKM120. BKM120 has anti-proliferative activity when acting on cell lines deregulated by PI3K, including A2780, U87MG, MCF7 and DU145, with GI50 of 0.1-0.7nM (Burger MT, et al.ACS Med Chem Lett, 2011,2(10), 774–779). BKM120 induces apoptosis in multiple myeloma cells (ARP1, ARK, MM.1S, MM1.R and U266), resulting in increased G1 phase cells and decreased S phase cells. BKM120 induces apoptosis in CD138+ primary MM cells and is less toxic to CD138- stromal cells. BKM120 can cause upregulation of BimS and downregulation of XIAP. (Zheng Y, et al. J Mol Med (Berl), 2011 Dec 30.) BKM120...

Claims

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