不对称合成丝氨酸蛋白酶凝血级联酶 FXIa 的硅二醇抑制剂。
Asymmetric Synthesis of Silanediol Inhibitors for the Serine Protease Coagulation Cascade Enzyme FXIa.
机构信息
Department of Chemistry , Hanoi National University of Education 136 Xuan Thuy Street , Cau Giay District, Hanoi , Vietnam.
Department of Chemistry , Temple University , 1901 North 13th Street , Philadelphia , Pennsylvania 19122 , United States.
出版信息
J Org Chem. 2018 May 18;83(10):5398-5409. doi: 10.1021/acs.joc.8b00116. Epub 2018 Apr 30.
Silanediol peptidomimetics have been prepared, designed to inhibit the serine protease enzyme Factor XIa (FXIa) for treatment of thrombosis without complete interruption of normal hemostasis. These Arg-[Si]-Ala analogues of the FXIa substrate (FIX) are the first silanediol dipeptide analogues to carry a basic guanidine group. Control of stereochemistry was accomplished using catalytic asymmetric hydrosilylation and addition of a silyllithium intermediate to the Davis-Ellman sulfinimine.
硅二醇肽拟肽已被制备，旨在抑制丝氨酸蛋白酶酶因子 XIa（FXIa），以治疗血栓而不完全中断正常止血。这些 FXIa 底物（FIX）的 Arg-[Si]-Ala 类似物是第一个带有碱性胍基的硅二醇二肽类似物。使用催化不对称氢化硅烷化和将硅烷基锂中间体加成到戴维斯-埃尔曼亚磺亚胺来控制立体化学。
Zotero 插件