申请人:Wave Life Sciences Ltd.
公开号:EP3248982A1
公开(公告)日:2017-11-29
Described herein are thiosulfonate reagents of Structure IIa useful for the synthesis of phosphorothiotriesters from H-phosphonates in a stereospecific fashion.
wherein,
X is alkyl, cycloalkyl, or heteroaryl;
R is R1-R2;
R1 is selected from -S-alkenylene-, -S-alkylene-, -S-alkylene-aryl-alkylene-, -S-CO-aryl-alkylene-, and -S-CO-alkylene-aryl-alkylene-; and
R2 is selected from heterocyclo-alkylene-S-, heterocyclo-alkenylene-S-,aminoalkyl-S-, and (alkyl)4N-alkylene-S-.
本文描述的是结构 IIa 的硫代磺酸试剂,可用于以立体特异性方式从 H-膦酸盐合成硫代磷酸酯。
其中
X 是烷基、环烷基或杂芳基;
R 是 R1-R2;
R1 选自-S-亚烷基、-S-亚烷基、-S-亚烷基-芳基-亚烷基、-S-CO-芳基-亚烷基和-S-CO-亚烷基-芳基-亚烷基;以及
R2 选自杂环亚烷基-S-、杂环亚烯基-S-、氨基烷基-S-和(烷基)4N-亚烷基-S-。