CAS: 26638-66-4; 3,11-Dichloro-6-Methyl-6,11-Dihydrodibenzo[c,F][1,2]Thiazepine 5,5-Dioxide

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CAS号26723-60-4 3-氯-6,11-二氢-6-甲... | CAS号26638-53-9 3-氯-6-甲基二苯并[c,f...

3-氯-6-甲基二苯并[c,F][1,2]硫氮杂卓-11(6H)-酮 5,5-二氧化物置于盐酸,Sodium Tetrahydroborate体系中,用 四氢呋喃,二氯甲烷 用作溶剂,化学反应生成3,11-二氯-6,11-二氢-6-甲基-二苯并[c,F][1,2]硫氮杂卓 5,5-二氧化物
参考文献:New Triazine Derivatives As Potent Modulators Of Multidrug Resistance
标题:New Triazine Derivatives As Potent Modulators Of Multidrug Resistance
摘要:A Series Of 70 Triazine Derivatives Have Been Synthesized And Tested For Their Capacity To Modulate Multidrug Resistance (Mdr) In Dc-3F/ad And Kb-A1 Tumor Cells In Vitro,In Comparison With Verapamil (Vrp),A Calcium Channel Antagonist Currently Used In Therapy As An Antihypertensive Drug,Which Also Shows Mdr Modulating Activity. Among The 12 Selected Compounds,16 (S9788) Showed High Mdr Reversing Properties In Vitro (300-And 6-Fold Vrp At 5-Mu-M In Dc-3F/ad And Kb-A1 Cells,Respectively) And Induced A Strong Accumulation Of Adriamycin. The Relationship Between The Increase Of Adr Accumulation And The Fold Reversal Induced By These Compounds And Their Lack Of Effects On The Sensitive Dc-3F Cells Suggest That They Act Mainly By Inhibiting The P-Glycoprotein (Pgp) Catalyzed Efflux Of Cytotoxic Agents,As Already Described For A Majority Of Mdr Modulators. In Vivo,In Association With The Antitumor Drug Vincristine (0.25 Mg/kg),16 (100 Mg/kg) Increased The Tic By 39% In Mice Bearing The Resistant Tumor Cell Line P388/vcr. According To These Interesting Properties,16 Was Selected For A Clinical Development Because It Was More Bioavailable Than 34,Even Though It Was Less Active.
Doi:10.1021/jm00091A017

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:FR-2807039-A1
优先权日:2000-03-31
标 题 :NOVEL 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: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: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

专利号:DE-60100321-T2
优先权日:2000-03-31
标题:A process for preparing 11-amino-3-chloro-6,11-dihydro-5,5-dioxo-6-methyldibenzo [c, f] [1,2] thiazepine and for use in the synthesis of thianeptine