A combinatorial scaffold approach based upon a multicomponent reaction.
A combinatorial scaffolding procedure for the synthesis and spatial arrangement of tripartite structures was developed. [reaction: see text]
Journal Article↗
Biomedical subjects
Roger Olsson
Publications and source records attributed to Roger Olsson.
One-pot three-component reaction for the synthesis of alpha-(aminoethyl)-alpha,beta-enones.
[reaction: see text] The synthesis of alpha-substituted alpha,beta-enones by a new metal iodide-promoted one-pot three-component reaction involving commercially available cyclopropyl ketones, aldehydes, and secondary amines followed by base treatment is described.
Journal Article↗
Discovery of the first nonpeptide agonist of the GPR14/urotensin-II receptor: 3-(4-chlorophenyl)-3-(2- (dimethylamino)ethyl)isochroman-1-one (AC-7954).
A functional cell-based screen identified 3-(4-chlorophenyl)-3-(2-(dimethylamino)ethyl)isochroman-1-one hydrochloride (AC-7954, 1) as a nonpeptidic agonist of the urotensin-II receptor. Racemic 1 had an EC50 of 300 nM at the human UII receptor and was highly selective. Testing of the enantiopure (+)- and (-)- 1 revealed that the UII receptor activity of racemic 1 resides primarily in (+)-1. Being a selective nonpeptidic druglike UII receptor agonist, (+)-1 will be useful as a pharmacological research tool and a potential drug lead.
Animals↗
A novel metal iodide promoted three-component synthesis of substituted pyrrolidines.
[reaction: see text] A new one-pot procedure for the synthesis of substituted pyrrolidine derivatives with commercially available cyclopropyl ketones, aldehydes, and amines by a metal iodide promoted three-component reaction was developed.
Aldehydes↗