158358-18-0Relevant academic research and scientific papers
Structure-activity relationship studies on benzofuran analogs of propafenone-type modulators of tumor cell multidrug resistance
Ecker,Chiba,Hitzler,Schmid,Visser,Cordes,Csollei,Seydel,Schaper
, p. 4767 - 4774 (1996)
A series of benzofurylethanolamine analogs of propafenone (1a) have been prepared and evaluated for multidrug resistance-reversing activity in two in vitro assay systems. As for propafenones, an excellent correlation of biological data with calculated lipophilicity values was found for benzofurans, whereby the latter generally had lower activity/lipophilicity ratios. Almost identical slopes of the regression lines were obtained for both propafenones and benzofurans. Multiple linear regression analysis of the complete data set yielded an equation with excellent predictive power (r2(cross-valid) = 0.968). Interaction measurements with artificial membranes indicated that the differences in activity between these two series of compounds are not due to differences in the interaction pattern with biological membranes.
Asymmetric synthesis of (S)-bufuralol and a propafenone analogue
Zaidlewicz, Marek,Tafelska-Kaczmarek, Agnieszka,Prewysz-Kwinto, Andrzej,Chechlowska, Aldona
, p. 1659 - 1664 (2007/10/03)
Asymmetric synthesis of (S)-bufuralol of 87% ee from 3-ethyl-2-hydroxybenzaldehyde, via the reduction of 2-bromo-1-(7-ethylbenzofuran-2-yl)ethanone with (-)-B-chlorodiisopinocampheylborane as the key step, followed by cyclization of the product bromohydrin to the corresponding epoxide and treatment with tert-butylamine, is described. (S)-1-(3-Phenethylbenzofuran-2-yl)-2-propylaminoethanol of 73% ee, a propafenone analogue, was prepared following the same approach.
