We report the first general conditions for the challenging Suzuki-Miyaura reaction with pyrrole-related sulfonate coupling partners (24 examples, 60-97%). Bis(dichloro)bis(2-dicyclohexylphosphino-2′,4′,6′-triiso-propylbiphenyl) palladium(II) precatalyst ensures the high efficiency of the reaction. The total synthesis of rhazinilam, a monoterpenoid indole alkaloid, highlights such cross-coupling as well as the simple preparation of pyrrolyl sulfonates by N-toO 1,5-sulfonyl migration catalyzed by gold(I) (15 examples, 54-93%).

The new hybrid NHC gold(I) acetonitrile polyoxometalate complexes {[Au(IPr)(MeCN) ][H ] [SiW O ] (1), [Au(IPr)(MeCN) ][H ] [PMo O ] (2), [Au(IPr)(MeCN) ][H ] [P W O ] (3), [Au(IPr)(MeCN) ][H ] [PW O ] (4), [Au(IPr)(MeCN) ] [PMo O ] (5) and [Au(ItBu)(MeCN) ] [H ] [PMo O ] (6)} were readily synthesized in high yield and characterized by NMR and MS-ESI spectroscopy. In a preliminary catalytic study, their activity was assessed under heterogeneous conditions for the ene-yne rearrangement reaction and a cycloisomerization reaction. Additionally, their reactivity and recyclability were tested in the hydration of alkynes under homogeneous conditions.

The purpose of this study was to synthesize a fluorine-18 labeled, highly selective aldosterone synthase ( h CYP11B2) inhibitor, [ 18 F]AldoView, and to assess its potential for the detection of aldosterone-producing adenomas (APAs) with positron emission tomography in patients with primary hyperaldosteronism (PHA). Using dibenzothiophene sulfonium salt chemistry, [ 18 F]AldoView was obtained in high radiochemical yield in one step from [ 18 F]fluoride. In mice, the tracer showed a favorable pharmacokinetic profile, including rapid distribution and clearance. Imaging in the adrenal tissue from patients with PHA revealed diffuse binding patterns in the adrenal cortex, avid binding in some adenomas, and “hot spots” consistent with aldosterone-producing cell clusters. The binding pattern was in good visual agreement with the antibody staining of h CYP11B2 and distinguished areas with normal and excessive h CYP11B2 expression. Taken together, [ 18 F]AldoView is a promising tracer for the detection of APAs in patients with PHA.