Klausen Rebekka S, Jacobsen Eric N
Department of Chemistry and Chemical Biology, Harvard University, 12 Oxford Street, Cambridge, Massachusetts 02138, USA.
Org Lett. 2009 Feb 19;11(4):887-90. doi: 10.1021/ol802887h.
The development of one-pot imine formation and asymmetric Pictet-Spengler reactions cocatalyzed by a chiral thiourea and benzoic acid is described. Optically active tetrahydro-beta-carbolines, ubiquitous structural motifs in biologically active natural products, are obtained in high ee directly from tryptamine and aldehyde precursors.
描述了在手性硫脲和苯甲酸共同催化下一锅法形成亚胺及不对称Pictet-Spengler反应的进展。光学活性的四氢-β-咔啉是生物活性天然产物中普遍存在的结构基序,可直接从色胺和醛前体以高对映体过量获得。