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Published on: February 16, 2018
Asymmetric Synthesis of Silanediol Inhibitors for the Serine Protease Coagulation Cascade Enzyme FXIa
Hoan Q Duong1, Scott McN Sieburth2
1Department of Chemistry , Hanoi National University of Education 136 Xuan Thuy Street , Cau Giay District, Hanoi , Vietnam.
Abstract:
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.
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