Chemoenzymatic synthesis of the potential antihypertensive agent (2R, 2′ S)-β-hydroxyhomometoprolol

…, A Torres-Gavilán, A López-Munguía, E Castillo

Index: Regla, Ignacio; Luviano-Jardon, Axel; Demare, Patricia; Hong, Enrique; Torres-Gavilan, Alejandro; Lopez-Munguia, Agustin; Castillo, Edmundo Tetrahedron Asymmetry, 2008 , vol. 19, # 21 p. 2439 - 2442

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Citation Number: 7

Abstract

The kinetic resolution of 1-chloro-3-[4-(2-methoxyethyl) phenoxy]-2-propanol rac-4 with Novozym 435 and vinyl stearate, a key step in the gram-scale synthesis of (2S)-2-[[(2R)-2- hydroxy-3-[4-(2-methoxyethyl) phenoxy] propyl] amino]-1-butanol (R, S)-1 a potent antihypertensive agent currently under investigation, is reported here. Our approach differs from the previously reported synthesis, which involves a tedious and poorly effective ...