Pandey Shashi, Kumar S Vinod, Kant Ruchir, Chauhan Prem M S
Medicinal and Process Chemistry Division, CSIR-Central Drug Research Institute, Sector 10, Jankipuram Extension, Sitapur Road, Lucknow 226031, India.
Org Biomol Chem. 2014 Aug 7;12(29):5346-50. doi: 10.1039/c4ob00793j.
A metal-free facile and efficient two-step synthetic protocol for the preparation of 1,4-benzoxazepine-5(2H)-one derivatives has been developed. The protocol involves Ugi reaction followed by K2CO3 mediated highly regioselective 7-exo-dig intramolecular cyclization of less-nucleophilic oxygen with the pendant alkyne moiety of an Ugi-propargyl precursor to afford the 1,4-benzoxazepine-5(2H)-one derivatives in good to excellent yields.
已开发出一种无金属的简便高效两步合成方案，用于制备1,4-苯并恶唑啉-5(2H)-酮衍生物。该方案包括Ugi反应，随后是碳酸钾介导的、亲核性较弱的氧与Ugi-炔丙基前体的侧链炔基部分进行的高度区域选择性7-外向-环化反应，从而以良好至优异的产率得到1,4-苯并恶唑啉-5(2H)-酮衍生物。
