A high-throughput synthesis of 1,2,4-oxadiazole and 1,2,4-triazole libraries in a continuous flow reactor

Bogdan Andrew R.; Wang Ying

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A high-throughput synthesis of 1,2,4-oxadiazole and 1,2,4-triazole libraries in a continuous flow reactor

机译：在连续流反应器中高通量合成1,2,4-恶二唑和1,2,4-三唑库

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We report herein a high-throughput methodology for the synthesis of 1,2,4-oxadiazole and 1,2,4-triazole small-molecule libraries using an integrated synthesis and purification platform. The heterocyclization relies first on a low-temperature peptide coupling of a diverse set of carboxylic acids and hydroxyamidines, hydrazonamides, or pyridyl hydrazides followed by a high-temperature cyclization to yield the respective heterocycles in a continuous flow process. The fully integrated synthesis and purification platform enables the rapid generation of chemical libraries, decreasing the drug discovery cycle time.

机译：我们在此报告了使用集成的合成和纯化平台合成1,2,4-恶二唑和1,2,4-三唑小分子文库的高通量方法。杂环化首先依赖于各种羧酸和羟am，肼基酰胺或吡啶基酰肼的低温肽偶联，然后进行高温环化以在连续流动过程中产生相应的杂环。完全集成的合成和纯化平台能够快速生成化学文库，从而缩短了药物发现周期的时间。

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《RSC Advances》 |2015年第97期|共6页
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Bogdan Andrew R.; Wang Ying;
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1. A high-throughput synthesis of 1,2,4-oxadiazole and 1,2,4-triazole libraries in a continuous flow reactor [J] . Bogdan Andrew R., Wang Ying RSC Advances . 2015,第97期

机译：在连续流反应器中高通量合成1,2,4-恶二唑和1,2,4-三唑库
2. Synthesis of 1,2,4-Triazoles, N-Fused 1,2,4-Triazoles and 1,2,4-Oxadiazoles via Molybdenum Hexacarbonyl-Mediated Carbonylation of Aryl Iodides [J] . Nakka Mangarao, Tadikonda Ramu, Nakka Srinivas, Advanced synthesis & catalysis . 2016,第4期

机译：六羰基钼介导的芳基碘化物羰基化反应合成1,2,4-三唑，N-稠合的1,2,4-三唑和1,2,4-恶二唑
3. SYNTHESIS OF 1,2,4-OXADIAZOLE-, 1,3,4-OXADIAZOLE-, AND 1,2,4-TRIAZOLE-DERIVED DIPEPTIDOMIMETICS [Review] [J] . Borg S., Luthman K., Csoregh I., The Journal of Organic Chemistry . 1995,第10期

机译：1,2,4-恶二唑-，1,3,4-恶二唑-和1,2,4-三唑衍生的拟双肽的合成[综述]
4. Synthesis and Evaluation of Poly(1,2,4-Triazole) and Poly(1,3,4-Oxadiazole)/H-3PO-4 Complexes [C] . Mamiko Kumagai, Yuko Takeoka, Masahiro Rikukawa ECS Meeting . 2003

机译：聚（1,2,4-三唑）和聚（1,3,4-恶二唑）/ H-3PO-4复合物的合成与评价
5. Development of new hypervalent iodine mediated reaction methodologies for cleavage of alkenes and synthesis of 1,2,4-oxadiazoles [D] . Sharma, Jhanvi. 2014

机译：新型高效碘介导的反应方法，用于切割烯烃和1,2,4-氧代唑的合成
6. Multicapillary Flow Reactor: Synthesis of 125-Thiadiazepane 11-Dioxide Library Utilizing One-Pot Elimination and Inter-/Intramolecular Double aza-Michael Addition Via Microwave-Assisted Continuous-Flow Organic Synthesis (MACOS) [O] . Farman Ullah, Qin Zang, Salim Javed, -1

机译：多功用流量反应器：使用微波辅助连续流动有机合成（MACOS）的单盆消除和/分子分子间双AZA-MICHAEL添加125-噻二亚哌己烷蛋白11-二氧化氮杂物库的合成
7. Rapid, microwave accelerated synthesis of 1,2,4triazolo3,4- b 1,3,4oxadiazoles from 4-acylamino-1,2,4-triazoles [O] . Stephanie L. Breunig, Margaret E. Olson, Daniel A. Harki 2016

机译：快速，微波加速合成1,2,4三唑唑3,4- b 1,3,4来自4-酰基氨基-1,2,4-三唑的氧基唑
8. 1,2,4-Triazoles and 1,3,4-Oxadiazoles from N-Acylhydrazidines [R] . Hergenrother, P. M., Pratt, T. J. 1969

机译：来自N-酰基肼的1,2,4-三唑和1,3,4-恶二唑

A high-throughput synthesis of 1,2,4-oxadiazole and 1,2,4-triazole libraries in a continuous flow reactor

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