A Concise Route to MK-4482 (EIDD-2801)

A two-step route to MK-4482 (EIDD-2801, <b>1</b>) was developed consisting of an esterification and hydroxamination of cytidine. The reactions can be conducted in either order with overall yields of 67% (first step—esterification) and 37% (first step—hydroxamination). Selective esterification of the nucleoside’s primary alcohol by enzymatic means eliminated the need for diol protection/deprotection, and direct transamination with hydroxylamine precluded the necessity of activating the nucleobase for amine coupling. This results in a significant advancement over the reported synthesis which is formed in at best 17% yield. The step count is reduced from five transformation to two, and the more expensive uridine is replaced with the more available cytidine.

A Concise Route to MK-4482 (EIDD-2801)

A two-step route to MK-4482 (EIDD-2801, <b>1</b>) was developed consisting of an esterification and hydroxamination of cytidine. The reactions can be conducted in either order with overall yields of 67% (first step—esterification) and 37% (first step—hydroxamination). Selective esterification of the nucleoside’s primary alcohol by enzymatic means eliminated the need for diol protection/deprotection, and direct transamination with hydroxylamine precluded the necessity of activating the nucleobase for amine coupling. This results in a significant advancement over the reported synthesis which is formed in at best 17% yield. The step count is reduced from five transformation to two, and the more expensive uridine is replaced with the more available cytidine.

Triacetin Production by Selective Esterification of Glycerol over Activated Zeolite and Lewatite as Catalyst

The conversion of glycerol as by product of biodiesel manufacture into value-added product was studied. Esterification of glycerol with acetic acid to triacetin was carried out using activated zeolite and Lewatite as catalyst A selective method for triacetin synthesis was developed to investigate the effect of molar ratio of glycerol to acetic acid (1:6, 1:7 and 1:8). The conversion values at the reactant mole ratio were subsequently 66.91%, 73.36% and 73.16%, while the selectivity obtained was 7.67%, 9.66% and 10.61% respectively. From these results, it can be concluded that the highest conversion was obtained at a reactant mole ratio of 1: 7 and the highest selectivity was obtained at a reactant mole ratio of 1: 8. The result of selectivity with various catalyst type shows that the Lewatit catalyst produces a higher selectivity than the use of activated natural zeolite as a catalyst.