CAS: 36016-39-4; Tert-Butyl ((Mesitylsulfonyl)Oxy)Carbamate

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CAS号773-64-8 2,4,6-三甲基苯磺酰氯 | CAS号36016-38-3 N-叔丁氧羰基羟胺 | CAS号36016-40-7 2-[(氨基氧基)磺酰]-1,...

均三甲苯置于氯磺酸,三乙胺体系中,用 甲基叔丁基醚,氯仿 作为反应溶剂,化学反应 3.0H,反应生成 N-Boc-O-2,4,6-三甲基苯磺酰羟胺
参考文献: N-(4-Fluorophenyl)-5-Phenyl-[1,2,4] Triazolo [1,5-A] Pyridine-2-Carboxamide Derivatives And Their Synthesis Thereof[fr] Dérivés De N-(4-Fluorophényl)-5-Phényl-[1,2,4]Triazolo[1,5-A]Pyridine-2-Carboxamide Et Leur Synthèse
标题: N-(4-Fluorophenyl)-5-Phenyl-[1,2,4] Triazolo [1,5-A] Pyridine-2-Carboxamide Derivatives And Their Synthesis Thereof[fr] Dérivés De N-(4-Fluorophényl)-5-Phényl-[1,2,4]Triazolo[1,5-A]Pyridine-2-Carboxamide Et Leur Synthèse
摘要:本发明涉及开发新型n-(4-氟苯基)-5-苯基-[1,2,4]三唑并[1,5-A]吡啶-2-羧酰胺衍生物,用于其不同的药理活性.特别涉及开发n-(4-氟苯基)-5-苯基-[1,2,4]三唑并[1,5-A]吡啶-2-羧酰胺衍生物作为抗病毒,抗癌,抗真菌,降糖,抗结核,镇静和抗2型糖尿病活性.具体涉及n-(4-氟苯基)-5-苯基-[1,2,4]三唑并[1,5-A]吡啶-2-羧酰胺衍生物用于治疗h37Rv和多药耐药(Mdr)分枝杆菌结核杆菌(Mtb)的方法.本发明还涉及n-(4-氟苯基)-5-苯基-[1,2,4]三唑并[1,5-A]吡啶-2-羧酰胺衍生物的合成方法.该发明还涉及治疗结核病,2型糖尿病,细菌,病毒和真菌感染的治疗方法.该发明通过发明新的反应方法论来解决化学过程和产品的挑战,最大程度地提高所需产品的产量,减少副产物,设计新的合成方案,简化化学生产操作,并寻找对环境和生态无害的无毒试剂.利用合成新型n-(4-氟苯基)-5-苯基-[1,2,4]三唑并[1,5-A]吡啶-2-羧酰胺衍生物来开发新的合成方法和其药理应用.设计合成了新系列n-(4-氟苯基)-5-苯基-[1,2,4]三唑并[1,5-A]吡啶-2-羧酰胺衍生物并评估了它们对h37Rv和多药耐药(Mdr)分枝杆菌结核杆菌(Mtb)的体外抗分枝杆菌活性.所有合成的化合物均通过质谱,核磁共振和元素分析等光谱方法进行表征.

专利信息

专利号:WO-2021161084-A1
优先权日:2020-02-16
标题 :N-(4-fluorophenyl)-5-phenyl-[1,2,4] triazolo [1,5-a] pyridine-2-carboxamide derivatives and their synthesis thereof
发明人：NINGEGOWDA RAGHU; BANUPRAKASH GOVINDAPPA; CHANDRASHEKHARAPPA SANDEEP
权利人:NINGEGOWDA RAGHU; BANUPRAKASH GOVINDAPPA; CHANDRASHEKHARAPPA SANDEEP
摘要:The present invention relates to the development of novel N-(4-fluorophenyl)-5-phenyl- [1,2,4]triazolo[1,5-a]pyridine-2-carboxamide derivatives for their different pharmacological activities. It particularly relates to the development of N-(4-fluorophenyl)-5-phenyl- [1,2,4]triazolo[1,5-a]pyridine-2-carboxamide derivatives as antiviral, anticancer, antifungal, hypoglycemic, anti-tubercular, sedative, anti-type 2 diabetes activity. It specifically relates to the N-(4-fluorophenyl)-5-phenyl-[1,2,4]triazolo[1,5-a]pyridine-2-carboxamide derivatives for treatment of H37Rv and multidrug-resistant (MDR) strains of Mycobacterium tuberculosis (MTB). The present invention also relates to the process for synthesis of N-(4-fluorophenyl)- 5-phenyl-[1,2,4]triazolo[1,5-a]pyridine-2-carboxamide derivatives. The invention further relates to method for treatment of method for treatment of diseases such as tuberculosis, type 2 diabetes, bacterial, viral and fungal infections. Invention addresses the challenges in working with chemical processes and products by inventing novel reaction methodology that can maximize the desired products and minimize by-products, designing new synthetic schemes that can simplify operations in chemical productions and seeking nontoxic reagent that are inherently environmentally and ecologically benign. Synthesis of novel N-(4- fluorophenyl)-5-phenyl-[1,2,4]triazolo[1,5-a]pyridine-2-carboxamide derivatives is being employed to develop a novel synthetic methodology and their pharmacological applications. Novel series of N-(4-fluorophenyl)-5-phenyl-[1,2,4]triazolo[l,5-a]pyridine-2-carboxamide derivatives were designed synthesized evaluated for their in vitro anti-mycobacterial activity against H37Rv and multi-drug-resistant (MDR) strains of mycobacterium tuberculosis (MTB). All the synthesized compounds were characterized by spectroscopic methods like Mass, NMR and elemental analysis.