合成含 MBX-4132 的 1,3,4-oxadiazole 的新型高效工艺,作为淋病奈瑟菌的抗菌剂

IF 1.8 3区 化学 Q3 CHEMISTRY, ORGANIC
Prachi Ramteke , M.S. Gill
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引用次数: 0

摘要

据报道,一种新颖高效的方法合成了 MBX-4132。这种含有 1,3,4-恶二唑的化合物通过与细菌核糖体结合来抑制反式翻译过程,并可作为一种抗菌剂。它涉及 5-(4-氟苯基)-1,3,4-恶二唑-2-胺与碳酸二苯酯的反应,生成相应的氨基甲酸酯,氨基甲酸酯与 1,2,3,4-四氢异喹啉原位反应生成 MBX-4132,产率相对较高(65%)。上述工艺的反应条件温和,使用碳酸二苯酯等无毒、无害、成本较低的试剂作为羰基源,因此既经济又环保。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Novel and efficient process for the synthesis of 1,3,4-oxadiazole containing MBX-4132 as antimicrobial agent in Neisseria gonorrhoeae
A novel and efficient approach to the synthesis of MBX-4132 has been reported. Having 1,3,4-oxadiazole-containing compound that inhibits trans translation process by binding to the bacterial ribosome and act as an antimicrobial agent. It involved the reaction of 5-(4-fluorophenyl)-1,3,4-oxadiazol-2-amine, with diphenyl carbonate to yield the corresponding carbamates, which in situ reacted with 1,2,3,4-tetrahydroisoquinoline to produce MBX-4132 with a comparatively higher yield (65%). The above process involves mild reaction conditions and uses nontoxic, non-hazardous, and cheaper reagents such as diphenyl carbonate as a carbonyl source thereby making the process economical and environment friendly.
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来源期刊
Synthetic Communications
Synthetic Communications 化学-有机化学
CiteScore
4.40
自引率
4.80%
发文量
156
审稿时长
4.3 months
期刊介绍: Synthetic Communications presents communications describing new methods, reagents, and other synthetic work pertaining to organic chemistry with sufficient experimental detail to permit reported reactions to be repeated by a chemist reasonably skilled in the art. In addition, the Journal features short, focused review articles discussing topics within its remit of synthetic organic chemistry.
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