期刊
ADVANCED SYNTHESIS & CATALYSIS
卷 355, 期 18, 页码 3517-3521出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/adsc.201300802
关键词
alkynes; continuous synthesis; copper; microreactor; trifluoromethyl ketones
资金
- Max-Plank Society
A copper(I)/N-heterocyclic carbene complex-catalyzed addition of terminal alkynes to trifluoromethyl ketones at low loading is described. The developed process functions well using a range of terminal alkynes but functions best when an aryl trifluoromethyl ketone is used. This substrate scope is well-suited for the production of active pharmaceutical ingredients (APIs) such as efavirenz. In this vein, we demonstrate that the described method can be translated into a flow process laying the framework for a completely continuous synthesis of efavirenz in the future.
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