CAS: 141645-16-1; (2-Butyl-5-Nitrobenzofuran-3-yl)(4-Hydroxyphenyl)Methanone

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2-羟基-5-硝基苄溴置于aluminum (III) Chloride,三苯基膦体系中,用 二氯甲烷,氯苯 用作溶剂,化学反应 30.0H,反应生成2-丁基-3-(4-羟基苯甲酰基)-5-硝基苯并呋喃
参考文献:发现决奈达隆及其类似物作为具有强效抗炎活性的 Nlrp3 炎症小体抑制剂
标题:发现决奈达隆及其类似物作为具有强效抗炎活性的 Nlrp3 炎症小体抑制剂
摘要:抑制 Nlrp3 炎症小体激活是治疗不受控制的炎症疾病的前瞻性治疗策略.这是第一次将多离子通道阻滞剂决奈达隆鉴定为 Nlrp3 炎症小体抑制剂,其抑制il-1 β释放的 Ic 50值为 6.84 μm .设计并合成了一系列新型 5-酰胺苯并呋喃衍生物作为 Nlrp3 炎症小体抑制剂.化合物 8C对 Il-1 β释放的活性略有增加(ic 50 = 3.85 μm).值得注意的是,用 8C 处理可以显着抑制 Nlrp3 介导的 Il-1 β在脓毒症小鼠模型中释放和改善腹膜炎症.总的来说,8C 是一种有前途的先导化合物,可作为具有抗炎作用的 Nlrp3 抑制剂进行进一步的化学开发.
Doi:10.1016/j.Bmcl.2021.128160

专利信息

专利号:US-2012108828-A1
优先权日:2010-09-09
标题 :Synthesis of dronedarone and salts thereof
发明人：SATHE DHANANJAY GOVIND; PATIL SAMADHAN DAULAT; GAIKWAD UMESH DILIP; RAO MANTRIPRAGADA NARAYANA; SHINDE AJIT BHASKAR
权利人:SATHE DHANANJAY GOVIND; PATIL SAMADHAN DAULAT; GAIKWAD UMESH DILIP; RAO MANTRIPRAGADA NARAYANA; SHINDE AJIT BHASKAR; USV LTD B S D MARG
摘要:The present invention relates to a process for preparation of Dronedarone or pharmaceutically acceptable salts thereof. More particularly, the present invention provides a process for preparation of Dronedarone hydrochloride, without the isolation of Dronedarone base.

专利号:US-8536350-B2
优先权日:2010-02-23
标 题:Process for the manufacture of dronedarone
发明人：SADA MARA; NARDI ANTONIO; MAIORANA STEFANO
权利人:SADA MARA; NARDI ANTONIO; MAIORANA STEFANO; LABORATORIO CHIMICO INT SPA
摘要:The invention relates to a new process for the preparation of dronedarone and its salts, in particular a synthesis process which allows said compound and its salts to be obtained with good yields, high purity and in an industrially expedient manner; the invention also concerns a new synthesis intermediate.

专利号:US-6828448-B2
优先权日:2000-12-11
标 题:Methanesulphonamido-benzofuran, preparation method and use thereof as synthesis intermediate
发明人：FINO NOEL; LEROY CORINNE
权利人:SANOFI SYNTHELABO
摘要:The invention relates to 2-butyl-5-(methanesulfonamido)benzofuran, its preparation and its use. n This compound is a synthesis intermediate, in particular for the preparation of dronedarone.

专利号:US-8779201-B2
优先权日:2007-10-02
标题 :Process for preparing benzofurans
发明人：EKLUND LARS
权利人:CAMBREX KARLSKOGA AB
摘要:There is provided a process for the preparation of a compound of formula (I), wherein R 1 , R 2 , R 3 , R 4 , X and Y are as described in the description. Such compounds may, for example, be useful intermediates in the synthesis of drugs such as Dronedarone.

专利号:EP-2428511-A1
优先权日:2010-09-09
标 题:Synthesis of dronedarone and salts thereof

专利号:CN-102659726-B
优先权日:2012-03-30
标题:Method for synthesis of dronedarone