A Machine-Assisted Flow Synthesis of SR48692: A Probe for the Investigation of Neurotensin Receptor-1

被引:60
作者
Battilocchio, Claudio [1 ]
Deadman, Benjamin J. [1 ]
Nikbin, Nikzad [1 ]
Kitching, Matthew O. [1 ]
Baxendale, Ian R. [2 ]
Ley, Steven V. [1 ]
机构
[1] Univ Cambridge, Dept Chem, Innovat Technol Ctr, Cambridge CB2 1EW, England
[2] Univ Durham, Dept Chem, Durham DH1 3LE, England
基金
英国工程与自然科学研究理事会;
关键词
batch processes; flow chemistry; medicinal chemistry; organic chemistry; synthetic methods; LINE IR-ANALYSIS; PROSTATE-CANCER; CHEMISTRY; MICROREACTORS; CELL; SEPARATION; MONOLITHS; REACTORS; POTENT; GREEN;
D O I
10.1002/chem.201300696
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
Here we report the direct comparison of a conventional batch mode synthesis of Meclinertant (SR48692, 1), a neurotensin receptor-1 antagonist, with its machine-assisted flow chemistry alternative. By using these enabling tools, combined with solid-supported reagents and scavengers, many process advantages were observed. Care, however, must be taken not to convert these techniques into expensive solutions to problems that do not exist.
引用
收藏
页码:7917 / 7930
页数:14
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