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Molecules 2017, 22(11), 1971;

Practical and Sustainable Synthesis of Optically Pure Levocabastine, a H1 Receptor Antagonist

College of Pharmacy, Seoul National University, 1 Gwanak-ro, Gwanak-gu, Seoul 08826, Korea
Department of Synthetic Chemistry, Chong Kun Dang Research Institute, 315-20, Dongbaekjukjeon-daero, Giheung-gu, Yongin-si 16995, Gyeonggi-do, Korea
College of Pharmacy, Cha University, 120 Haeryong-ro, Pocheon 11160, Gyeonggi-do, Korea
Author to whom correspondence should be addressed.
Received: 23 October 2017 / Accepted: 11 November 2017 / Published: 15 November 2017
(This article belongs to the Section Organic Chemistry)
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A practical and sustainable method for the synthesis of levocabastine hydrochloride (1), a H1 receptor antagonist for the treatment of allergic conjunctivitis, that can be applied to the industrial production of the compound has been developed. Substantial improvements over the previously reported procedure are achieved via efficient preparation of an optically active key intermediate (5) without chiral resolution and with a more effective detosylation, which complements the previous procedure. Notably, our process requires no chromatographic purification and provides levocabastine hydrochloride in greater than 99.5% purity in a 14.2% overall yield. View Full-Text
Keywords: levocabastine; anti-histamine; H1 receptor antagonist levocabastine; anti-histamine; H1 receptor antagonist

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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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Kang, S.K.; Nam, D.H.; Ahn, J.; Lee, J.; Sim, J.; Lee, J.; Suh, Y.-G. Practical and Sustainable Synthesis of Optically Pure Levocabastine, a H1 Receptor Antagonist. Molecules 2017, 22, 1971.

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