[EN] IMPROVED AMINOHYDROXYLATION OF ALKENES<br/>[FR] AMINOHYDROXYLATION AMÉLIORÉE D'ALCÈNES
申请人:IND RES LTD
公开号:WO2011159177A1
公开(公告)日:2011-12-22
The invention relates to a process for the aminohydroxylation of alkenes using N-oxycarbamate reagents, e.g. N-acyloxycarbamate, N-alkyloxycarbonyloxycarbamate and N-aralkoxycarbonyloxycarbamate reagents. The invention particularly relates to an intermolecular aminohydroxylation reaction that can be carried out in the absence of added base. The invention also relates to novel N-oxycarbamate reagents that are stable crystalline materials. The process of the invention is useful in the synthesis of compounds having a vicinal amino alcohol moiety, such as biologically active compounds.
该发明涉及一种使用N-氧羰酸酯试剂(例如N-酰氧羰酸酯、N-烷氧羰酸酯和N-芳基氧羰酸酯试剂)对烯烃进行氨羟基化的方法。该发明特别涉及一种可以在无需添加碱的情况下进行的分子间氨羟基化反应。该发明还涉及新颖的N-氧羰酸酯试剂,这些试剂是稳定的结晶材料。该发明的方法在合成具有邻位氨基醇基团的化合物方面非常有用,例如具有生物活性的化合物。