CAS: 26638-53-9; 3-Chloro-6,11-Dihydro-6-Methyl-5,5,11-Trioxodibenzo[c,F][1,2]Thiazepine

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CAS号26638-66-4 rac 3,11-二氯-6,1... | CAS号26723-60-4 3-氯-6,11-二氢-6-甲...

2-(N-Methyl-N-Phenyl-Aminesulfonyl)-4-Chloro Benzoic Acid置于aluminum (III) Chloride,氯化亚砜体系中,用 1,2-二氯乙烷 用作溶剂,化学反应 2.0H,反应生成3-氯-6-甲基二苯并[c,F][1,2]硫氮杂卓-11(6H)-酮 5,5-二氧化物
参考文献:治疗甲型h1N1流感病毒的巴洛沙韦马波西尔类似物的合成及生物学评价
标题:治疗甲型h1N1流感病毒的巴洛沙韦马波西尔类似物的合成及生物学评价
摘要:流感病毒的 Rna 依赖性 Rna 聚合酶 (Rdrp) 由 Pa,Pb1 和 Pb2 蛋白的亚基组成,负责病毒 Mrna 转录和 Vrna 复制.帽依赖性核酸内切酶 (Cen) 存在于 Rdrp 的 Pa 亚基中,介导病毒 Rna 转录的关键"帽抢夺"步骤,被认为是一个有前途的抗流感靶点.在这份手稿中,设计,合成和生物学研究了一系列作为 Cen 抑制剂的新型化合物.研究了目标化合物对甲型/h 1 N 1流感病毒的细胞活性,并总结了构效关系 (Sar).结果表明,某些化合物对流感 A/h 1 N 1具有活性ic 50值小于 100 μm 的病毒.微粒体代谢稳定性在人,猴子和大鼠物种中进行,结果表明化合物32和40的活性成分足够稳定,可以进行体内研究.体内药代动力学结果表明,化合物32对于 Ig 和 Iv 给药均具有可接受的生物学参数.然后在balb/c小鼠中进行化合物32的体内毒性研究,剂量为100和50
Doi:10.1002/jhet.4546

专利信息

专利号:US-6441165-B2
优先权日:2000-03-31
标 题:Process for the preparation of 11-amino-3-chloro-6, 11-dihydro-5, 5-dioxo-6-methyl-dibenzo[c,f][1,2]thiazepine and application to the synthesis of tianeptine
发明人：BLANCHARD JACKY; TURBE HUGUES; BRIGOT DANIEL
权利人:SERVIER LAB
摘要:Process for the industrial synthesis of the compound of formula (I):and its addition salts.Application to the synthesis of tianeptine and its pharmaceutically acceptable salts.

专利号:EP-1138677-B1
优先权日:2000-03-31
标 题 :Process for the preparation of 11-amino-3-chloro-6,11-dihydro-5,5-dioxo-6-methyl-dibenzo[c,f][1,2]-thiazepine and application to the synthesis of tianeptine

专利号:NO-318088-B1
优先权日:2000-03-31
标题:New Process for the Preparation of 11-Amino-3-Chloro-6,11-Dihydro-5,5-Dioxo-6-Methyl-Dibenzo [c, f] [1,2] Thiazepine and Application to the Synthesis of Thianeptin

专利号:US-2001037021-A1
优先权日:2000-03-31
标 题 :Process for the preparation of 11-amino-3-chloro-6,11-dihydro-5,5-dioxo-6-methyl-dibenzo[c,f][1,2]thiazepine and application to the synthesis of tianeptine

专利号:AU-3336801-A
优先权日:2000-03-31
标题:New process for the preparation of 11-amino-3-chloro-6,11- dihydro-5,5-dioxo-6-methyl-dibenzo(c,f)(1,2)thiazepine and application to the synthesis of tianeptine

专利号:EP-1138677-A1
优先权日:2000-03-31
标 题 :Process for the preparation of 11-amino-3-chloro-6,11-dihydro-5,5-dioxo-6-methyl-dibenzo[c,f][1,2]-thiazepine and application to the synthesis of tianeptine