Department of Chemistry, Merck and Co., Inc., 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, USA.
Org Lett. 2010 Mar 5;12(5):1116-9. doi: 10.1021/ol100119e.
The oxetane ring is useful in drug discovery as a bioisostere for both the geminal dimethyl group and the carbonyl group. A convenient, straightforward approach to access structurally diverse 3-aminooxetanes through the reactivity of oxetan-3-tert-butylsulfinimine and the corresponding sulfinylaziridine is described.
氧杂环丁烷环在药物发现中可用作偕二甲基和羰基的生物等排体。本文描述了通过氧杂环丁-3-叔丁基亚磺酰亚胺和相应的亚磺酰基氮丙啶的反应性,来获得结构多样的 3-氨基氧杂环丁烷的一种方便、直接的方法。