A coupled chlorinase–fluorinase system with a high efficiency of trans-halogenation and a shared substrate tolerance

Abstract

Enzymatic trans-halogenation enables radiolabeling under mild and aqueous conditions, but rapid reactions are desired. We developed a coupled chlorinase–fluorinase system for rapid trans-halogenation. Notably, the chlorinase shares a substrate tolerance with the fluorinase, enabling these two enzymes to cooperatively produce 5′-fluorodeoxy-2-ethynyladenosine (5′-FDEA) in up to 91.6% yield in 1 h.