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Chroman derivative and preparation method and application thereof
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A derivative, the technology of chroman, applied in the field of pharmacy, achieves the effects of novel structure, excellent ACC inhibitory activity and broad development prospects
Active Publication Date: 2019-03-01
CHINA PHARM UNIV
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[0005] At present, the research on ACC inhibitors at home and abroad is in the clinical and preclinical research stage, and no drug has been approved for marketing. It is necessary to study compounds with more diverse structural types to obtain ideal drugs.
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[0088] Put 8g (52.80mmol) of 2,4-dihydroxyacetophenone and 150mL of 1,4-dioxane into a 250mL three-necked flask, and stir at room temperature until completely dissolved. Add 11.20 mL (0.11 mol) borontrifluorideether solution drop by drop, and stir at room temperature until the solution turns pink. Then, 7.19 g (0.11 mol) of isoprene in 1,4-dioxane (25 mL) was added dropwise, and the solution turned purple-black, and stirred overnight at room temperature. After the reaction was detected by TLC, saturated ammoniumchloride solution (50mL) was added to the reaction solution, extracted with ethyl acetate (60mL×3), the organic phases were combined, and the organic phase was washed with saturated sodiumchloride solution (50mL). It was dried over sodium sulf...
[0099] The synthesis procedure was the same as in Example 1, and 69 mg of white solid was obtained, with a melting point of 219-221° C. and a yield of 77%.
[0100] 1 H NMR (300MHz, DMSO-d 6 )δ13.05(s,1H),8.35–8.21(m,1H),7.87–7.69(m,3H),7.60(d,J=9.1Hz,3H),7.50(s,1H),7.25(d ,J=8.3Hz,1H),6.34(s,1H),4.21(s,2H),3.69(s,2H),2.81–2.64(m,4H),1.92(s,2H),1.84–1.71( m,4H),1.29(s,6H).MS(ESI)m / z: calculated for C 32 h 31 N 3 o 4 [M-H] - :520.2, found: 520.2.
[0104] The synthesis steps were the same as in Example 1, and 70 mg of white solid was obtained, with a melting point of 175-177° C. and a yield of 70%.
[0105] 1 H NMR (300MHz, DMSO-d 6 )δ12.19(s,1H),7.49(s,1H),7.34(s,1H),6.98(s,1H),6.33(s,1H),4.17(s,2H),2.80(t,J =7.5Hz,2H),2.72(d,J=8.9Hz,4H),2.49(s,3H),2.01–1.63(m,8H),1.29(s,6H),0.94(t,J=7.4Hz ,3H).MS(ESI)m / z: calculated for C 30 h 35 N 3 o 4 [M+Na] + :524.3,found:524.3.
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Abstract
The invention discloses a chroman derivative. The structure of the chroman derivative is shown in a formula (I) (Please see the specifications for the formula (I)). According to the chroman derivative, the structure is novel, excellent ACC inhibitory activity and non-alcoholic fatty liverdisease resisting activity in vivo are achieved, and transcription of fatty acid from de novo synthesis genes,inflammation related genes and liver fibrosis related genes can be significantly lowered; and intestinal microecology disturbance induced by high-fat food can be further improved. The chroman derivative and medicinal salt thereof can be used for treating or preventing non-alcoholic fatty liverdisease, alcoholic fatty liverdisease and metabolic syndromes, excellent drug safety is shown, and broad development prospects are achieved.
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