Synthesis and cardiovascular activity of metoprolol analogues

R Melgar-Fernandez, P Demare, E Hong…

Index: Melgar-Fernandez, Roberto; Demare, Patricia; Hong, Enrique; Rosas, Miguel Angel; Escalante, Jaime; Munoz-Muniz, Omar; Juaristi, Eusebio; Regla, Ignacio Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 1 p. 191 - 194

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Citation Number: 4

Abstract

The synthesis of four novel analogues of metoprolol, a well-known β1-blocker used to reduce arterial blood pressure, is described. The preparation of (2S, 2′ S)-7,(2R, 2′ S)- 7,(2R, 2′ R)-8, and (2S, 2′ R)-8 was based on the reaction of racemic 2-[4-(2′- methoxyethyl)-phenoxymethyl]-oxirane (4) with (R)-or (S)-2-amino-1-butanol. Salient characteristics of analogues 7 and 8 relative to metoprolol are the incorporation of an ...