Abstract:Biocatalytic methodology has been developed for the efficient and environment friendly synthesis of 3′-O,4′-C-methylene-linked α-l-arabinonucleosides.
“…In the past few years, several works about the enzyme-catalyzed synthesis of uridine esters were reported. [29][30][31][32][33][34][35][36] Some lipase such as CAL-B 22 and pseudomonas cepacia lipase 29 have been applied to the synthesis of uridine esters, but it requires a longer reaction time (24 h) to achieve the desired result. Flow chemistry especially catalyst/substrate conditions in continuous-ow systems can increase the reactivity and selectivity.…”
We achieved the effective controllable regioselective acylation of the primary hydroxyl group of uridine derivatives catalyzed by Lipase TL IM from Thermomyces lanuginosus with excellent conversion and regioselectivity.
“…In the past few years, several works about the enzyme-catalyzed synthesis of uridine esters were reported. [29][30][31][32][33][34][35][36] Some lipase such as CAL-B 22 and pseudomonas cepacia lipase 29 have been applied to the synthesis of uridine esters, but it requires a longer reaction time (24 h) to achieve the desired result. Flow chemistry especially catalyst/substrate conditions in continuous-ow systems can increase the reactivity and selectivity.…”
We achieved the effective controllable regioselective acylation of the primary hydroxyl group of uridine derivatives catalyzed by Lipase TL IM from Thermomyces lanuginosus with excellent conversion and regioselectivity.
A two-step route to MK-4482 (EIDD-2801, 1) was developed consisting of an esterification and hydroxamination of cytidine. The selective acylation and direct amination eliminate the need for protecting and activating...
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