期刊
ORGANIC & BIOMOLECULAR CHEMISTRY
卷 13, 期 44, 页码 10888-10894出版社
ROYAL SOC CHEMISTRY
DOI: 10.1039/c5ob01801c
关键词
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资金
- Pfizer
- Engineering and Physical Sciences Research Council (EPSRC)
- University College London Department of Chemistry
- Engineering and Physical Sciences Research Council [EP/E052789/1, EP/K004840/1, 1353678] Funding Source: researchfish
- EPSRC [EP/K004840/1, EP/E052789/1] Funding Source: UKRI
The use of B(OCH2CF3)(3) for mediating direct amidation reactions of a wide range of pharmaceutically relevant carboxylic acids and amines is described, including numerous heterocycle-containing examples. An initial screen of solvents for the direct amidation reaction suggested that cyclopentyl methyl ether, a solvent with a very good safety profile suitable for use over a wide temperature range, was an excellent replacement for the previously used solvent acetonitrile. Under these conditions amides could be prepared from 18 of the 21 carboxylic acids and 18 of the 21 amines examined. Further optimisation of one of the low yielding amidation reactions (36% yield) via a design of experiments approach enabled an 84% yield of the amide to be obtained.
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