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1 article(s) from Bräuner-Osborne, Hans

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

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Figure 1: Marketed calcium-sensing receptor agonist cinacalcet (1), and CaSR antagonists Calhex 231 (2) and N...

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Scheme 1: Strategy for assembling (R)-3 from fragments 4, 5 and 6. m-Ns = m-nitrobenzenesulfonyl.

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Scheme 2: Synthesis of amine building block 6 by using Katritzky’s pyrylium chemistry [16].

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Scheme 3: Synthesis of phenol 4 from commercially available aryl fluoride 13.

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Scheme 4: Synthesis of rac-3 and (R)-3 from commercially available racemic- and (S)-glycidol 15, respectively...

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Figure 2: Determination of the optical purity for (R)-3 by chiral HPLC on a Daicel AD-H column. Top: Opticall...

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Figure 3: Characterisation of concentration-dependent (R)-3 inhibition of 3.5 mM calcium-stimulated IP₁ respo...

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Published 09 Jul 2013

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