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A hydroxamic acid derivative of phthalazinone and its preparation method and application
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A technology of hydroxime and phthalazinone, applied in the field of phthalazinone hydroxamic acid derivatives and preparation thereof, can solve the problems of complex pharmacokinetics, interaction, toxic and side effects, etc.
Active Publication Date: 2019-07-26
深圳贝瑞生物医药科技有限公司
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However, there are disadvantages such as complex pharmacokinetics, possible drug interactions, and more toxic side effects in combination drugs, and a single small molecule with multi-target inhibitory activity can effectively avoid these problems, and the development of multi-target inhibitors has become an important issue. A common drug development strategy
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[0057] 4-Bromophenethylamine (10g, 50mmol) was dissolved in 250ml of dichloromethane, di-tert-butyl dicarbonate (12g, 55mmol) was added, stirred at room temperature for 3 hours, followed by saturated ammoniumchlorideaqueous solution, saturated carbonic acid The reaction liquid was washed with aqueous sodiumhydrogen solution, water, and saturated brine, and the organic phase was dried over anhydrousmagnesiumsulfate and spin-dried to obtain a crude product. Crystallization from diethyl ether afforded the title compound (white solid, 14.70 g, 98% yield). 1 H NMR (400MHz, Chloroform-d) δ7.42 (d, J = 8.4Hz, 2H), 7.07 (d, J = 8.3Hz, 2H), 4.51 (s, 1H), 3.35 (br, 2H), 2.75 (t,J=7.0Hz,2H),1.43(s,9H).
[0061] Example 1A (3.0g, 10mmol), anhydrouspotassiumcarbonate (2.764g, 20mmol), a catalytic amount of ditriphenylphosphine palladium dichloride were placed in a 50ml round bottom flask, and dimethylformamide (DMF) was added Methyl acrylate (1.8 ml, 20 mmol) was added after deoxygenating in vacuo and replacing with nitrogen. React overnight at 120-130°C. After the reaction was completed, water was added and extracted with ethyl acetate. The organic phase was dried over anhydrousmagnesiumsulfate, spin-dried, and washed with deionized water to obtain the title compound (white solid, 2.53 g, 83% yield). 1 H NMR (400MHz, Chloroform-d) δ7.68(d, J=16.0Hz, 1H), 7.47(d, J=7.8Hz, 2H), 7.22(d, J=7.8Hz, 2H), 6.42(d ,J=16.1Hz,1H),4.59(s,1H),3.81(s,3H),3.43–3.31(m,2H),2.82(t,J=7.0Hz,2H),1.34(s,9H) .
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technical field [0001] The invention belongs to the field of medicine, and in particular relates to a phthalazinone hydroxamic acid derivative with PARP and HDAC inhibitory activity and a preparation method and application thereof. Background technique [0002] Polyadenosine diphosphate-ribosepolymerase (PARP) can catalyze the polyadenosine diphosphate-ribosesylation of substrate proteins. The currently known PARP family contains 17 subtypes, of which PARP1 and PARP2 are DNA-dependent and can Activated by broken DNA strands. PARP1 plays a key role in the repair of DNA single-strand breaks and is an important target for the development of anti-tumor drugs. At present, the clinical development of PARP1 inhibitors mainly includes combination therapy and monotherapy: (1) Since PARP1 inhibitors can block the repair of DNA damage by tumor cells, combining PARP1 inhibitors with radiation that can cause DNA damage The combination of therapy or DNA toxic agents can enhance the sen...
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