AMRI Hungary Zrt., Záhony u. 7., Budapest, 1035, Hungary.
Mol Divers. 2012 Feb;16(1):81-90. doi: 10.1007/s11030-012-9357-2. Epub 2012 Jan 26.
An efficient and convenient solution-phase synthesis of a 1H-1,2,4-triazole library with potential agrochemical activity is reported employing microwave-assisted organic synthesis (MAOS) and continuous-flow microfluidic synthetic methods starting from commercially available 3,5-dibromo-1H-1,2,4-triazole (1). MAOS was used for the synthesis of 5-amino-3-bromo-1,2,4-triazole analogs 3 and for their 3-aryl derivatives 4 via Suzuki-Miyaura coupling with polymer-supported catalyst. A microfluidic hydrogenation reactor integrated into an automated parallel synthesis platform was built and utilized for the reductive dehalogenation reactions providing 5-aminotriazoles (5).
报道了一种采用微波辅助有机合成（MAOS）和连续流动微流合成方法，从商业可得的 3,5-二溴-1H-1,2,4-三唑（1）出发，高效便捷地合成具有潜在农用化学品活性的 1H-1,2,4-三唑文库的方法。MAOS 用于合成 5-氨基-3-溴-1,2,4-三唑类似物 3，并通过与聚合物负载催化剂的 Suzuki-Miyaura 偶联反应合成其 3-芳基衍生物 4。构建了一个集成到自动化平行合成平台中的微流氢化反应器，并用于还原脱卤反应，提供 5-氨基三唑（5）。
