A rapid construction of THIQs by a Pd(II)-catalyzed C(sp)-H olefination of free primary and secondary 2-phenylethylamines with high step- and atom-economy was reported. Notably, no substituent was required at the α-position to the amino group of the 2-phenylethylamines. The substrate scope was broad, and the reaction could also be applied to generate THIQs from the biologically active molecules such as the drug molecule baclofen and phenylalanine ester.
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| http://dx.doi.org/10.1021/acs.joc.9b01769 | DOI Listing |
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