作者:Matilda Duffy、Mara Di Filippo、Marcus Baumann
DOI:10.1016/j.tetlet.2021.153522
日期:2021.12
A continuous flow protocol is reported for the synthesis of 2H-indazoles via the thermal Cadogan reaction. Triethyl phosphite serves as a readily available deoxygenation reagent providing a facile entry to a series of drug-like 2H-indazoles in high chemical yields. Compared to an analogous batch approach, the flow process was advantageous as it provides for a contained environment where boiling of
报道了通过热卡多根反应合成 2 H-吲唑的连续流动方案。亚磷酸三乙酯作为一种容易获得的脱氧试剂,可以以高化学产率轻松进入一系列类似药物的 2 H-吲唑。与类似的分批方法相比,流动过程是有利的,因为它提供了一个封闭的环境,在这个环境中,通过使用背压调节器 (BPR) 来抑制试剂的沸腾,这反过来又会导致更快的动力学。直接放大提供了数克数量的 2 H-吲唑,其通过光驱动和区域特异性乙酰化的进一步功能化在流动模式下得到了证明。