High throughput screening identified a phenoxyacetic acid scaffold as a novel CRTh2 receptor antagonist chemotype, which could be optimised to furnish a compound with functional potency for inhibition of human eosinophil shape change and oral bioavailability in the rat.
Regioselective alkylation of phenol with cyclopentanol over montmorillonite K10: An efficient synthesis of l-(2-cyclopentylphenoxy)-3-[(l,l-dimethylethyl)amino]propan-2-ol {(S')-penbutolol}
Regioselective alkylation of phenol with cyclopentanol is achieved over Montmorillonite K10 clay, producing 2-cycIopentylphenol, the key intermediate. The synthesis of optically active (S)-penbutoIol 1, an important antihypertensive drug, is realized in 5 steps from 2-cyclopentylphenol by employing Sharpless asymmetric dihydroxylation. The Royal Society of Chemistry 1999.
Phukan, Prodeep,Sudalai, Arumugam
p. 3015 - 3018
(2007/10/03)
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