Synthesis of the calcilytic ligand NPS 2143

• Henrik Johansson,
• Thomas Cailly,
• Alex Rojas Bie Thomsen,
• Hans Bräuner-Osborne and
• Daniel Sejer Pedersen

Beilstein J. Org. Chem. 2013, 9, 1383–1387, doi:10.3762/bjoc.9.154

• optical purity (er > 99:1) as demonstrated by chiral HPLC and the pharmacological profile for (R)-3 is in full accordance with that reported in the literature. Keywords: epoxides; GPCR; NPS 2143; nucleophilic aromatic substitution; pyrylium chemistry; Introduction The first G-protein-coupled receptors

• cells stably transfected with rat CaSR. The graph is representative of three independent experiments. Strategy for assembling (R)-3 from fragments 4, 5 and 6. m-Ns = m-nitrobenzenesulfonyl. Synthesis of amine building block 6 by using Katritzky’s pyrylium chemistry [16]. Synthesis of phenol 4 from