486437-19-8Relevant articles and documents
Development of a telescoped flow process for the safe and effective generation of propargylic amines
Donnelly, Kian,Zhang, Huan,Baumann, Marcus
, (2019/11/02)
Propargylic amines are important multifunctional building blocks that are frequently exploited in the synthesis of privileged heterocyclic entities. Herein we report on a novel flow process that achieves the safe and effective on-demand synthesis of propargylic amines in a telescoped manner. This process minimizes exposure to hazardous azide intermediates and renders a streamlined route into these building blocks. The value of this approach is demonstrated by the rapid generation of a small selection of drug-like thiazolines that result from a high-yielding reaction cascade between propargylic amines with different aryl isothiocyanates.