Reissert Indole Synthesis Using Continuous-Flow Hydrogenation

被引:21
|
作者
Colombo, Eloic [1 ]
Ratel, Philippe [1 ]
Mounier, Laurent [1 ]
Guillier, Fabrice [1 ]
机构
[1] Labs Fournier SA, Chem Design & Synth Unit, F-21310 Daix, France
关键词
heterogeneous catalysis; reduction; Reissert indole synthesis; heterocycle; design of experiments; MICROREACTOR TECHNOLOGY; HIGH-PRESSURE; REACTOR; CONSTRUCTION; CYCLIZATION; CHEMISTRY; DESIGN;
D O I
10.1556/jfchem.2011.00009
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
A series of substituted indole-2-carboxylic acid ethyl esters and aza-indole analogs have been prepared using continuous-flow hydrogenation. The identification of some key parameters using a design of experiments (DoE)-based approach allowed efficient optimization of each synthesis. The scale-up study for the multigram preparation of one model indole substrate showed the importance of working at steady state with the H-Cube apparatus. A new useful method for the easy preparation of substituted indoles in various quantities is presented.
引用
收藏
页码:68 / U62
页数:45
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