Nobuta Tomoya, Xiao Guozhi, Ghislieri Diego, Gilmore Kerry, Seeberger Peter H
Max Planck Institute of Colloids and Interfaces, Am Mühlenberg 1, 14476 Potsdam, Germany.
Chem Commun (Camb). 2015 Oct 21;51(82):15133-6. doi: 10.1039/c5cc06093a. Epub 2015 Sep 1.
Five active pharmaceutical ingredients (APIs) containing the vicinyl amino alcohol moiety were synthesized using a convergent chemical assembly system. The continuous system is composed of four flow reaction modules: biphasic oxidation, Corey-Chaykovsky epoxidation, phenol alkylation, and epoxide aminolysis. Judicious choice of reagents and module order allowed for two classes of β-amino alcohols, aryl and aryloxy, to be synthesized in good (27-69%) overall yields.
使用一种汇聚化学组装系统合成了五种含有乙烯基氨基醇部分的活性药物成分(API)。该连续系统由四个流动反应模块组成:双相氧化、Corey-Chaykovsky环氧化、苯酚烷基化和环氧化物氨解。通过明智地选择试剂和模块顺序,可以以良好的总收率(27-69%)合成两类β-氨基醇,即芳基和芳氧基β-氨基醇。