作者
Sylvain Gauthier, Brigitte Caron, Julie Cloutier, Yves L Dory, Alexandre Favre, Denis Larouche, Josée Mailhot, Carl Ouellet, Annette Schwerdtfeger, Gilles Leblanc, Céline Martel, Jacques Simard, Yves Mérand, Alain Bélanger, Claude Labrie, Fernand Labrie
发表日期
1997/7/4
期刊
Journal of medicinal chemistry
卷号
40
期号
14
页码范围
2117-2122
出版商
American Chemical Society
简介
Scheme 1a a Reagents and conditions:(a) resorcinol, BF3 ‚Et2O (8.5 equiv), 100 C, 1 h (70% yield);(b) DHP (9.8 equiv), TsOH (catalytic amount), 0 C, 2.5 h (69% yield);(c)(i) 4-hydroxybenzaldehyde (1.04 equiv), piperidine (0.3 equiv), benzene, reflux, 60 h;(ii) 1-(2-chloroethyl) piperidine monohydrochloride (1.2 equiv), Cs2CO3 (2.4 equiv), acetone, H2O (1.4%), reflux, 19 h (65% yield);(d)(i) MeLi (3.0 equiv), THF,-78 C to room temperature, 3 h;(ii) AcOH, H2O (10%), 90 C, 0.5 h (60% yield);(e) HPLC chiral separation with a Chiralpak AD column;(f) PvCl (2.2 equiv), Et3N (2.5 equiv), CH2Cl2, 0 C to room temperature, 2 h (80% yield).
引用总数
学术搜索中的文章
S Gauthier, B Caron, J Cloutier, YL Dory, A Favre… - Journal of medicinal chemistry, 1997