Graczyk Karolina, Haven Tobias, Ackermann Lutz
Institut für Organische und Biomolekulare Chemie, Georg-August-Universität Göttingen, Tammannstraße 2, 37077 Göttingen (Germany) http://www.ackermann.chemie.uni-goettingen.de/
Institut für Organische und Biomolekulare Chemie, Georg-August-Universität Göttingen, Tammannstraße 2, 37077 Göttingen (Germany) http://www.ackermann.chemie.uni-goettingen.de/.
Chemistry. 2015 Jun 8;21(24):8812-5. doi: 10.1002/chem.201501134. Epub 2015 May 7.
The so-called magic methyl effect significantly boosts the bioactivities and physical properties of pharmacologically active drugs. Direct introduction of the methyl group by CH activation was accomplished with a versatile iron catalyst, which enabled the CH methylation of (hetero)benzamides, anilides, alkenes, and even alkanes by triazole assistance in a chemo-, site- and diastereo-selective fashion.
所谓的神奇甲基效应显著提高了药理活性药物的生物活性和物理性质。通过一种通用的铁催化剂实现了通过CH活化直接引入甲基,该催化剂能够在化学、位点和非对映选择性方面通过三唑辅助实现(杂)苯甲酰胺、酰苯胺、烯烃甚至烷烃的CH甲基化。