无金属[3+2]环加成反应：糖基烯基酯与原位生成的 CFCHN 的反应——CF 取代的吡唑啉糖缀合物的合成。
Metal-free [3+2] cycloaddition of glycosyl olefinic ester with in situ generated CFCHN: Access to CF-substituted pyrazoline glycoconjugates.
机构信息
Medicinal and Process Chemistry Division, CSIR-Central Drug Research Institute, BS-10/1, Sector 10, Jankipuram Extension, Sitapur Road, P.O. Box 173, Lucknow, 226 031, India.
Medicinal and Process Chemistry Division, CSIR-Central Drug Research Institute, BS-10/1, Sector 10, Jankipuram Extension, Sitapur Road, P.O. Box 173, Lucknow, 226 031, India; Academy of Scientific and Innovative Research, New Delhi, 110001, India.
出版信息
Carbohydr Res. 2020 Sep;495:108080. doi: 10.1016/j.carres.2020.108080. Epub 2020 Jul 6.
An efficient [3 + 2] cycloaddition of glycosyl olefinic ester with in situ generated CFCHN for the syntheses of CF-substituted pyrazoline glycoconjugate has been developed. This mild, one-pot reaction condition avoiding the use of metallic catalyst and additive will be useful in the pharmaceutical industry. This reaction features are the broad substrate scope, good functional group tolerance with good to high yields.
发展了一种通过糖苷烯基酯与原位生成的 CFCHN 的高效[3+2]环加成反应来合成 CF 取代的吡唑啉糖缀合物的方法。这种温和、一锅法的反应条件避免了使用金属催化剂和添加剂，在制药工业中将会很有用。该反应具有广泛的底物范围、良好的官能团耐受性和良好到高产率的特点。
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