Dadiboyena Sureshbabu, Nefzi Adel
Torrey Pines Institute for Molecular Studies, 11350 SW Village Parkway Port St. Lucie FL 34987 USA.
Tetrahedron Lett. 2012 Apr 18;53(16):2096-2099. doi: 10.1016/j.tetlet.2012.02.041.
An efficient approach for the parallel solid phase synthesis of isoxazole and isoxazoline derivatives has been developed. The isoxazoles and isoxazolines were constructed through a 1,3-dipolar cycloaddition reaction of nitrile oxides, with resin-bound alkynes or alkenes. The cycloaddition reaction conditions performed on solid phase supports was optimized, and an array of resin bound carboxylic acid building blocks were utilized for distinct conversions. This methodology presents a new alternative to the diversity oriented synthesis of disubstituted isoxazoles and isoxazolines different from existing routes which are limited in structural diversity.
已开发出一种用于异恶唑和异恶唑啉衍生物平行固相合成的有效方法。异恶唑和异恶唑啉是通过腈氧化物与树脂结合的炔烃或烯烃的1,3-偶极环加成反应构建的。对在固相载体上进行的环加成反应条件进行了优化，并利用一系列树脂结合的羧酸结构单元进行不同的转化。这种方法为二取代异恶唑和异恶唑啉的多样性导向合成提供了一种新的替代方法，不同于现有结构多样性有限的路线。
