N- versus O-arylation of aminoalcohols: Orthogonal selectivity in copper-based catalysts
Two complementary protocols for copper-catalyzed arylation of aminoalcohols were developed. Selective N-arylation was accomplished at room temperature using 2-isobutyrylcyclohexanone (a β-diketone) as supporting ligand, while selective O-arylation require
Shafir, Alexandr,Lichtor, Phillip A.,Buchwald, Stephen L.
p. 3490 - 3491
(2008/01/01)
Piperidylalkylindoles. 1. Hypotensive activity of 3-[2-(phenoxypiperidyl)ethyl]indoles
A series of 3-[2-(phenoxypiperidyl)ethyl]indoles was synthesized and evaluated for hypotensive activity in the spontaneous hypertensive rat. Maximum hypotensive activity appeared when the phenoxy substituent was para substituted and occupied the 4 position of the piperidine ring.
Helsley,Strupczewski,Woodward
p. 309 - 312
(2007/10/05)
Method of treating pain and hypertension
3-[2-(Phenyloxycycloazalkyl)ethyl]indoles possessing antihypertensive, analgesic, and tranquilizing properties and process for their preparation are described.
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(2008/06/13)
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