Synthesis of (R)-Olodaterol

T. Bouyssou; C. Hoenke; K. Rudolf; P. Lustenberger; S. Pestel; P. Sieger; R. Lotz; C. Heine; F. H. Büttner; A. Schnapp; I. Konetzki

doi:10.1055/s-0029-1219649

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Synfacts 2010(5): 0506-0506
DOI: 10.1055/s-0029-1219649

Synthesis of Natural Products and Potential Drugs

Synthesis of (R)-Olodaterol

Contributor(s): Philip Kocienski
T. Bouyssou, C. Hoenke, K. Rudolf, P. Lustenberger, S. Pestel, P. Sieger, R. Lotz, C. Heine, F. H. Büttner, A. Schnapp, I. Konetzki*
Boehringer Ingelheim Pharma GmbH & Co., Biberach, Germany

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Publication History

Publication Date:
22 April 2010 (online)

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Significance

Olodaterol is a potent agonist of the human β₂-adrenoceptor with a high β₁/β₂ selectivity. Its crystalline hydrochloride salt is suitable for inhalation and is currently undergoing clinical trials in man for the treatment of asthma. Olodaterol has a duration of action that exceeds 24 hours in two preclinical animal models of bronchoprotection and it has a better safety margin compared with formoterol.