It is challenging to develop simple and low cost catalytic systems while maintaining high reactivity and selectivity. An iron-catalyzed intramolecular C−H amination of sulfamate esters using simple and cheap ligands is reported with general substrate scope (31 examples, up to 95% yield). The addition of second ligand, bipyridine, is able to accelerate the reaction and increase the yield. The ready availability of these iron catalysts provides a promising approach to selective introduction of nitrogen into hydrocarbon feedstock.

An efficient strategy for N/O-(deutero)­alkylation of indoles and phenols with alkoxides/alcohols as the alkylation reagents is described. The consecutive detosylation/alkylation transformations feature mild reaction conditions, high ipso-selectivity, and good functional group tolerance (>50 examples). A one-pot selective N-alkylation of unprotected indoles with alcohols and TsCl is also realized. The application of this method is demonstrated by the introduction of isotope-labeled (CD3 and 13CH3) groups using the readily accessible labeled alcohols and the synthesis of pharmaceuticals.

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A New Route for the Synthesis of Ozagrel Hydrochloride. -Starting from p-tolualdehyde, a new cost efficient synthetic route to title compound (VI), a highly selective thromboxane A2 inhibitor, is described. The overall yield is 72% compared to 34% realized in a previously reported method. -(YU, C.; ZHAO, B.; ZHAO, Y.; LIN*, J.; Org.