📜Isopropyl ((2S,4R)-1-Acetyl-6-Bromo-2-Methyl-1,2,3,4-Tetrahydroquinolin-4-yl)Carbamate置于四(三苯基膦)钯,Bis(Dibenzylideneacetone)-Palladium(0),2-二环己膦基-2'-(N,N-二甲胺)-联苯 Aluminum (III) Chloride,水,Sodium Hydroxide,Sodium T-Butanolate体系中,用 乙二醇二甲醚,乙醇,二氯甲烷,甲苯 用作溶剂,化学反应 25.01H,反应生成4-[(2S,4R)-1-乙酰基-4-[(4-氯苯基)氨基]-2-甲基-1,2,3,4-四氢-6-喹啉基]苯甲酸 参考文献: Thetrahydroquinolines Derivatives As Bromodomain Inhibitors[fr] Dérivés De Tétrahydroquinolines Convenant Comme Inhibiteurs Du Bromodomaine 标题: Thetrahydroquinolines Derivatives As Bromodomain Inhibitors[fr] Dérivés De Tétrahydroquinolines Convenant Comme Inhibiteurs Du Bromodomaine 摘要:公式(i)的四氢喹啉化合物或其盐,含有这种化合物的药物组合物及其在治疗中的应用,特别是在溴结构域抑制剂适用于治疗的疾病或症状.
专利号:CN-118754894-A 优先权日:2024-07-26 标题 :JQ1 derivative containing o-naphthoquinone structure, synthesis method thereof and application of JQ1 derivative in preparation of anti-triple-negative breast cancer drugs
专利号:CN-118812557-A 优先权日:2024-07-26 标 题:BRD4/GPX4 double-target inhibitor, synthesis method thereof and application of inhibitor in preparation of triple-negative breast cancer therapeutic drug
1: Chan KH, Zengerle M, Testa A, Ciulli A. Impact of target warhead and linkage vector on inducing protein degradation: comparison of Bromodomain and Extra-Terminal (BET) degraders derived from triazolodiazepine (JQ1) and tetrahydroquinoline (I-BET726) BET inhibitor scaffolds. J Med Chem. 2017 Jun 8. doi: 10.1021/acs.jmedchem.6b01912. [Epub ahead of print] doi: 10.1021/jm5010539. Epub 2014 Sep 24. doi: 10.1371/journal.pone.0072967. eCollection 2013.
合成参考文献
参考文献:10.1055/s-0034-1379642 摘要:Synthesis of GSK1324726A. Synfacts. 2014 Dec 15;11(01):0002. doi: 10.1055/s-0034-1379642.