Bejan Vasilichia, Moldoveanu Costel, Mangalagiu Ionel I
Al. I. Cuza University of Iasi, Organic and Biochemistry Department, Bd. Carol 11, 700506 Iasi, Romania.
Ultrason Sonochem. 2009 Mar;16(3):312-5. doi: 10.1016/j.ultsonch.2008.10.012. Epub 2008 Nov 5.
A new, fast, efficient and general method for preparation of steroid analogous of anticipated biological activity under ultrasound irradiation and classical heating is reported. The reaction pathway involves two steps: quaternization of phthalazine heterocycle followed by a 3+2 dipolar cycloaddition of cycloimmonium ylides to dienophiles. Under ultrasound the reaction time decreases substantially, the yields are higher, the reaction conditions are milder. A comparative study ultrasound verses classical heating has been done.
报道了一种在超声辐射和传统加热条件下制备具有预期生物活性甾体类似物的新的、快速、高效且通用的方法。反应途径包括两个步骤：酞嗪杂环的季铵化，随后环亚胺叶立德与亲双烯体进行3+2偶极环加成反应。在超声作用下，反应时间大幅缩短，产率更高，反应条件更温和。已对超声和传统加热进行了对比研究。
