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Benzo lactone compounds and application thereof in preparation of anti-aids medicines
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A technology for benzolactones and compounds, applied in the preparation of anti-AIDS drugs, in the field of benzolactone compounds, can solve the problems of complex structure, difficult synthesis, not particularly good activity and the like
Active Publication Date: 2014-08-13
WUHAN UNIV
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The structure of flavonoids is relatively simple and has certain excellent physiological activities. It is the core skeleton structure of many drugs. Recently, it has been reported in the literature that chromones have certain anti-HIV reverse transcriptase activity, but most of them have complex structures and are difficult to synthesize. , and the activity is not particularly good, which limits the possibility of its medicine
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[0041] Take 0.2mmol of the carboxylic acid derivative of reaction i and 0.24mmol (1.2eq.) of 1,3-dichloro-5,5-dimethylhydantoin (DCDMH) into a single-necked round-bottomed flask containing a magnet Add 5mL of dichloromethane to dissolve it, stir evenly, add 0.02mmol of triethylenediamine (DABCO) to catalyze the halide lactonization reaction, and monitor the reaction by TLC. After the basic reaction of the raw materials was completed, the pure solid compound HX1 was obtained by column chromatography separation, and the product was a yellow solid with a yield of 71%. 1 H NMR (400MHz, CDCl 3 )δ8.17(d, J=7.7Hz, 1H), 7.68(d, J=7.2Hz, 1H), 7.61(d, J=7.6Hz, 1H), 7.55(d, J=7.6Hz, 1H) , 7.36(t, J=7.1Hz, 4H), 5.62(d, J=7.5Hz, 1H), 5.33(d, J=7.5Hz, 1H). 13 C NMR (101MHz, CDCl 3 )δ163.16, 137.65, 135.28, 134.83, 134.29, 130.55, 129.79, 129.20, 128.99, 128.49, 127.50, 127.11, 123.79, 83.36, 56.2...
Embodiment 2
[0042] Example 2: Preparation of 3-(chloro(3-toluene)methyl)isobenzofuran-1(3H)(HX2)
[0043] The preparation method was as in Example 1, and the product was a white solid with a yield of 83%. 1 H NMR (400MHz, CDCl 3 )δ8.17(d, J=7.7Hz, 1H), 7.64(d, J=7.4Hz, 1H), 7.58(d, J=7.6Hz, 1H), 7.51(t, J=7.5Hz, 1H) ,7.25(d,J=6.2Hz,1H),7.15(dd,J=18.1,7.5Hz,3H),5.65(d,J=6.7Hz,1H),5.39(d,J=6.7Hz,1H) ,2.34(s,3H). 13 C NMR (101MHz, CDCl 3 )δ163.38, 138.59, 137.79, 135.74, 134.65, 130.44, 130.01, 129.70, 128.60, 127.60, 127.56, 124.05, 84.13, 56.33, 21.47.
[0045] The preparation method was as in Example 1, and the product was a white solid with a yield of 87%. 1 H NMR (400MHz, CDCl 3 )δ8.17(d, J=7.7Hz, 1H), 7.70–7.66(m, 1H), 7.61(d, J=7.5Hz, 1H), 7.54(t, J=7.5Hz, 1H), 7.38– 7.32(m,4H),5.62(d,J=7.5Hz,1H),5.33(d,J=7.5Hz,1H). 13 C NMR (101MHz, CDCl 3 )δ163.15, 137.66, 135.29, 134.82, 134.29, 130.56, 129.79, 129.20, 128.99, 128.49, 127.49, 127.11, 123.80, 83.36, 56.27.
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Abstract
The invention belongs to the technical field of medicines, and particularly relates to a benzo lactone compounds and application thereof in preparation of anti-aids medicines.A series of benzo pentabasic lactone compounds and benzo hexa-lactone compounds are prepared from styrenecarboxylic acid derivatives and a halogenated reagent through an alkali-induced iodolactonisation, and the benzo lactone compounds are relatively similar to existing anti-aids medicines (such as efavirenz) and anti-aids active compounds (chromone derivatives). The invention mainly introduces the structures and preparation method of the compounds, as well as application of the compounds in preparation of the anti-aids medicines.
Description
technical field [0001] The invention belongs to the technical field of medicine, and relates to a benzolide compound and its application in preparing anti-AIDS drugs. Background technique [0002] AIDS (AIDS), the full name of Acquired Immunodeficiency Syndrome, is a very harmful infectious disease caused by HIV infection. The latest figures from World Guardian show that about 3 million people worldwide have died from AIDS, and there are still 30 million patients who are still struggling with AIDS. Human immunodeficiencyvirus type 1 (HIV-1) is the pathogenic factor causing acquired immunodeficiency syndrome. After the virus infects the host, it mainly uses reverse transcriptase, integrase and protease to complete its replication cycle. Because HIV is constantly mutating during the replication process, it has brought huge challenges to the development of drugs and vaccines. At present, the combination of several drugs with different mechanisms of action is mainly used clin...
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