Graduate School of Pharmaceutical Sciences, Tohoku University, 6-3 Aza-Aoba, Aramaki, Aoba-ku, Sendai 980-8578, Japan.
Org Lett. 2011 Sep 2;13(17):4526-9. doi: 10.1021/ol2016934. Epub 2011 Aug 3.
Regioselective cyclization of o-alkynoylphenols forming γ-benzopyranones has been demonstrated. Trifluoromethanesulfonic acid (TfOH) induced 6-endo cyclization of o-alkynoylphenols without forming 5-exo cyclized benzofuranone derivatives to provide the corresponding γ-benzopyranones in high yields.
邻炔基苯酚的区域选择性环化形成γ-苯并吡喃酮已经得到证实。三氟甲磺酸(TfOH)诱导邻炔基苯酚的 6-endo 环化,而不形成 5-exo 环化的苯并呋喃酮衍生物,以高产率提供相应的γ-苯并吡喃酮。