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Gamma-secretase inhibitor and use thereof
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A technology of n-cf3 and compounds, applied in the fields of active ingredients of heterocyclic compounds, nervous system diseases, organic chemistry, etc., can solve problems such as limited clinical benefits
Inactive Publication Date: 2014-03-26
李振 +1
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Clinical benefit with most currently available anticancer drugs is limited due to resistance and toxicity (eg, hematologic, hepatotoxicity, nephrotoxicity, and neurotoxicity) that develop during treatment
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[0026]
[0027] Key intermediates:
[0028]
[0029] Among them, A, B, and C are purchased directly, and D is obtained by hydrolysis of C in sodiumhydroxide water-methanol solution.
[0032] Add 1.29g of intermediate D, 1.57g of bromofluoromethane, and 2.01g of triethylamine into a 50mL single-necked bottle, add 10ml of dichloromethane and stir to dissolve, stir at room temperature overnight, remove the yellow precipitate by suction filtration, wash with water, and dry the organic phase with magnesiumsulfate. Compound 1.28g of compound 1-A purified by column chromatography. Yield 80%.
[0033] Put 1.25g of compound B in a 50mL single-necked bottle, add 10mL to dissolve, add 1.20g of compound 1-A, 2.06g of dicyclohexylcarbodiimide, 0.73g of 1-hydroxybenzotriazole, stir at room temperature for 3h, and remove by suction Off-white powder, concentrated filtrate, purified by column chromatography, EA:PE=3:1, to obtain off-white solid;
[0034] H-NMR: 3.670(3H, s), 7.2-7.9(8H, ddd), 2.251(1H, m), 2.122(1...
[0038] The experimental procedure is the same as in Example 1, and bromofluoromethane is replaced by bromotrifluoromethane, and the compound shown in the title is obtained after preparation and purification.
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Abstract
The invention relates to compound as shown in a formula (I) or pharmaceutically acceptable salts, optically pure antipodes, racemic modifications, prodrugs or derivatives thereof, wherein R1 is H or CH3, R2 is C1-3 alkyl, -(CR'R'')n-CF3, -(CR'R'')n-CHF2, -(CR'R'')n-CH2F or -(CH2)n-halogen, and n is 0 to 2 and optionally substituted by one or more substituents selected from halogen or CF3, aryl, and substituted aryl; R3 and R4 independently are H, halogen and C1-3 alkyl.
Description
technical field [0001] The present invention relates to compounds, which are inhibitors of γ-secretase and which are useful in the treatment or prevention of diseases associated with γ-secretase, such as tumors. Background technique [0002] Cancer is one of the deadliest diseases in the world. For most tumors, there remains a high rate of recurrence and metastasis associated with a very poor prognosis. Currently available drugs include cytotoxic chemotherapy, anti-angiogenic agents, and targeted agents. Clinical benefit with most currently available anticancer drugs is limited due to resistance and toxicity (eg, hematologic, hepatotoxicity, nephrotoxicity, and neurotoxicity) that develop during treatment. [0003] Cancer is a disease characterized by uncontrolled proliferation. Intensive research into the signaling pathways that drive cancer has revealed that tumors harbor a population of stem-like cells that differentiate into bulk cells with proliferative properties. ...
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