Breakthrough in the challenging P450-catalyzed chemoenzymatic synthesis of C14-functionalized steroids

摘要

Intensive past research has demonstrated that cytochrome P450 monooxygenases are involved in the biosynthesis of numerous natural products and in human metabolism of various pharmaceuticals [1]. This inspired synthetic organic and pharmaceutical chemists to test them as catalysts in the oxidative hydroxylation of steroids. Unfortunately, wildtype P450s generally proved to show low levels of regio-and diastereoselectivity as well as suboptimal activity.