CAS: 608523-94-0; N-Tert-Butyl 3-Aminophenylsulfonamide

上下游产品

3-nitrobenzenesulphonyl chloride N-(tert-butyl)-3-((2-chloro-5-methylpyrimidin-4-yl)amino)benzenesulfonamide 3-methyl-N-(3-sulfamoylphenyl)-L-valyl-(4R)-4-((7-chloro-4-methoxy-1-isoquinolinyl)oxy)-N-((1R,2S)-1-((cyclopropylsulfonyl)carbamoyl)-2-vinylcyclopropyl)-L-prolinamide N-(3-(tert-butylsulfamoyl)phenyl)-3-methyl-L-valyl-(4R)-4-((7-chloro-4-methoxy-1-isoquinolinyl)oxy)-N-((1R,2S)-1-((cyclopropylsulfonyl)carbamoyl)-2-vinylcyclopropyl)-L-prolinamide

📜3-硝基苯磺酰氯置于palladium 10% On Activated Carbon,一水合肼体系中,用 四氢呋喃,甲醇 作为反应溶剂,化学反应 8.0H,反应生成 N-叔丁基-3-氨基苯磺酰胺
参考文献:新型 Jak2/brd4(Bd2) 双靶点抑制剂嘌呤衍生物的设计,合成及生物学评价
标题:新型 Jak2/brd4(Bd2) 双靶点抑制剂嘌呤衍生物的设计,合成及生物学评价
摘要:基于 Jak2 和 Brd4置于nf-Kb 通路中的药理协同作用以及 Jak2 和 Brd4 抑制剂联合治疗 Mpn 和炎症的积极疗效.设计,制备了一系列选择性抑制 Janus 激酶 2 (Jak2) 和 Brd4(Bd2) 的独特 9 H-嘌呤-2,6-二胺衍生物,并评估了它们的体外和体内效力.其中,化合物9J表现出可接受的抑制活性,对brd4和jak2的bd2的ic 50值分别为13和22Nm.蛋白质印迹分析表明,9J在 Nf-Kb 通路中表现出非常好的功能效力,并且 P65,IKb-α 和 Ikkα/β 信号强度的磷酸化在 Raw264.7 细胞系上受到抑制.此外,9J显着改善了 Ba/f3-Jak2 V617F同种异体移植模型中的疾病症状.同时,9J也能有效缓解急性溃疡性结肠炎模型的症状.总之,9J是一种有效的 Jak2/brd4(Bd2) 双靶点抑制剂,可能是治疗骨髓增生性肿瘤和炎症性疾病的潜在先导化合物.
DOI:10.1016/j.Bioorg.2023.106386

专利信息

专利号:WO-2022269384-A1
优先权日:2021-06-24
标 题 :A process for the direct synthesis of fedratinib intermediate
发明人：DESAI ASIM HEMANTBHAI; PATIL SANJAY NIMBAJI; RADADIYA VAIBHAV GOVINDBHAI; DESAI JIGNASU THAKORBHAI; DUBEY RAJEEV RAMCHANDRA; CHOUBEY Ajit Kumar
权利人:AMI ORGANICS LTD
摘要:The present disclosure relates to a process for the direct synthesis of Fedratinib intermediate. Particularly, the present disclosure relates to a process for the direct synthesis of 3-amino-N- (tert-butyl)benzene sulfonamide. The process of the present disclosure has various advantages such as convenient operation conditions, time-saving process, easy purification, low operation costs, good yield and efficiency hence the process is industrially feasible. The use of non-toxic, inexpensive and easily available reagents, in the process of the present disclosure, makes the process cost-efficient economic and environmental friendly.

专利号:CN-114645068-A
优先权日:2020-12-21
标题 :A kind of enzyme-catalyzed synthesis method of aromatic amine compounds