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Beilstein-Institut, Beilstein Journal of Organic Chemistry, (9), p. 1383-1387, 2013

DOI: 10.3762/bjoc.9.154

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Synthesis of the calcilytic ligand NPS 2143

Journal article published in 2013 by Henrik Johansson, Thomas Cailly, Alex Rojas Bie Thomsen, Hans Bräuner-Osborne ORCID, Daniel Sejer Pedersen ORCID, Daniel Sejer Pedersen
This paper is made freely available by the publisher.
This paper is made freely available by the publisher.

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Abstract

(R)-3 (NPS 2143) is a negative allosteric modulator of the human calcium-sensing receptor (CaSR) and as such represents an important pharmacological tool compound for studying the CaSR. Herein, we disclose for the first time a complete experimental description, detailed characterisation and assessment of enantiomeric purity for (R)-3. An efficient, reproducible and scalable synthesis of (R)-3 that requires a minimum of chromatographic purification steps is presented. (R)-3 was obtained in excellent 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.