Ghorai Manas K, Sayyad Masthanvali, Nanaji Yerramsetti, Jana Sourita
Department of Chemistry, Indian Institute of Technology Kanpur, Kanpur, 208016, India.
Chem Asian J. 2015 Jul;10(7):1480-9. doi: 10.1002/asia.201500153. Epub 2015 May 14.
A simple protocol for the synthesis of dihydrobenzothiazines through regio- and stereoselective S(N)2-type ring opening of N-tosylaziridines with sulfur nucleophiles followed by copper-powder-mediated intramolecular C-N cyclization in excellent yields (up to 95%) with high diastereo- and enantioselectivity (up to >99%) is reported.
报道了一种简单的合成二氢苯并噻嗪的方法,该方法通过N - 对甲苯磺酰基氮丙啶与硫亲核试剂进行区域和立体选择性的S(N)2型开环反应,然后经铜粉介导的分子内C - N环化反应,以高达95%的优异产率以及高达>99%的高非对映选择性和对映选择性实现。