Namba Kosuke, Shoji Isamu, Nishizawa Mugio, Tanino Keiji
Division of Chemistry, Graduate School of Science, Hokkaido University, Kita-ku, Sapporo 060-0810, Japan.
Org Lett. 2009 Nov 5;11(21):4970-3. doi: 10.1021/ol9021194.
An efficient and simple method for selective acylation of either one of two nitrogen atoms of tosylhydrazide was developed. The selectivity was drastically controlled by a catalytic amount of 4-aminopyridine or 4-(dimethylamino)pyridine with common acylating agents. The nitrogen atom masked with a tosyl group was acylated in the presence of 4-aminopyridine, whereas the primary nitrogen atom was acylated in the absence of 4-aminopyridine.
开发了一种高效且简单的方法用于对甲苯磺酰肼的两个氮原子之一进行选择性酰化。通过使用催化量的4-氨基吡啶或4-（二甲基氨基）吡啶与常见的酰化剂可严格控制选择性。在4-氨基吡啶存在下，被甲苯磺酰基保护的氮原子发生酰化反应，而在没有4-氨基吡啶时，伯氮原子发生酰化反应。
