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Hydrolytic Enzymes for the Synthesis of Pharmaceuticals
Published in Peter Grunwald, Pharmaceutical Biocatalysis, 2019
Sergio González-Granda, Vicente Gotor-Fernández
Ramatroban is commercialised in Japan with the trade name Baynas® for treatment of asthma, coronary diseases and rhinitis, residing its main activity in the (R)-enantiomer (Scheme 9.28, bottom). The selective acylation of a key precursor, namely racemic 2,3,4,9-tetrahydro-1H-carbaz-3-ol was possible using 3 equiv. of vinyl acetate and CAL-B in dry THF (Busto et al., 2012), yielding both the (R)-acetate and the (S)-alcohol in enantiopure form at 30°C after 8 h (Scheme 9.28, top). In similar conditions, the stereoselective acylation of a Frovatriptan precursor was reported (Busto et al., 2013), drug with high affinity for human 5-HT1B and 5-HT1D receptors. The combination of 3 equiv. of vinyl acetate and CAL-B in THF allowed the synthesis of the corresponding enantiopure (R)-acetate and the (S)-alcohol (Scheme 9.28, middle). Lipase-catalysed acetylation reactions of indole derivatives for the asymmetric synthesis of (R)-Ramatroban and (R)-Frovatriptan.
Ramatroban for chemoprophylaxis and treatment of COVID-19: David takes on Goliath
Published in Expert Opinion on Therapeutic Targets, 2022
Kate C. Chiang, John G. Rizk, Deanna J. Nelson, Lakshmanan Krishnamurti, Selvakumar Subbian, John D. Imig, Imran Khan, Srinivasa T. Reddy, Ajay Gupta
In contrast to the shortcomings of therapeutic agents in the classes described above, ramatroban is an orally bioavailable, potent, dual TxA2/TP and PGD2/DP2 receptor antagonist, with demonstrated efficacy in a variety of animal models of respiratory inflammation, atherosclerosis, thrombosis, and sepsis [10]. The safety profile of ramatroban is well established, and the drug has been used in Japan over the past 20 years to treat allergic rhinitis [10].