Department of Analytical Biochemistry, Groningen Research Institute of Pharmacy, University of Groningen, A Deusinglaan 1, 9713 AV Groningen, The Netherlands.
Molecules. 2022 May 20;27(10):3293. doi: 10.3390/molecules27103293.
-dealkylation, the removal of an -alkyl group from an amine, is an important chemical transformation which provides routes for the synthesis of a wide range of pharmaceuticals, agrochemicals, bulk and fine chemicals. -dealkylation of amines is also an important in vivo metabolic pathway in the metabolism of xenobiotics. Identification and synthesis of drug metabolites such as -dealkylated metabolites are necessary throughout all phases of drug development studies. In this review, different approaches for the -dealkylation of amines including chemical, catalytic, electrochemical, photochemical and enzymatic methods will be discussed.
脱烷基化,即从胺中去除 -烷基基团,是一种重要的化学转化,为广泛的药物、农化品、大宗和精细化学品的合成提供了途径。胺的脱烷基化也是异生物质代谢中体内代谢途径的重要组成部分。在药物开发研究的所有阶段,都需要识别和合成药物代谢物,如脱烷基化代谢物。在这篇综述中,将讨论包括化学、催化、电化学、光化学和酶法在内的不同的胺脱烷基化方法。