Adamczyk M, Grote J
Department of Chemistry, Abbott Diagnostics Division, Abbott Laboratories, Abbott Park, Illinois 60064, USA.
Steroids. 1996 Oct;61(10):562-4. doi: 10.1016/s0039-128x(96)00113-4.
Pure 3 alpha- and 3 beta-aminodigoxigenin were previously prepared from 12-acetyldigoxigenin by a multistep route involving tosylation, azide inversion, deprotection, and reduction. This paper describes the straightforward synthesis of the pure epimers in a single step via reductive amination of digoxigenone and chromatographic separation without the need for protection and deprotection.
纯的3α-和3β-氨基洋地黄毒苷元先前是通过多步路线由12-乙酰基洋地黄毒苷元制备的,该路线涉及甲苯磺酰化、叠氮化物转化、脱保护和还原。本文描述了通过洋地黄毒苷元的还原胺化反应一步直接合成纯差向异构体并通过色谱分离,无需进行保护和脱保护。