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Synthesis of the calcilytic ligand NPS 2143.


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.

SUBMITTER: Johansson H 

PROVIDER: S-EPMC3740522 | biostudies-literature | 2013

REPOSITORIES: biostudies-literature

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Synthesis of the calcilytic ligand NPS 2143.

Johansson Henrik H   Cailly Thomas T   Rojas Bie Thomsen Alex A   Bräuner-Osborne Hans H   Sejer Pedersen Daniel D  

Beilstein journal of organic chemistry 20130709


(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 excell  ...[more]

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