One kind of net synthesis englitazone

2016 
The present invention provides a method for synthesizing species englitazone net, comprising: 2,3,4,6-tetra -O- benzyl-1,5-lactone -D- glucopyranose acid and p-chloro-iodobenzene as starting material, reaction intermediate of formula II; reductive elimination hydroxyl group on the anomeric carbon intermediates shown in formulas II, to give the intermediate of formula III; in (S) -3- phenoxy tetrahydrofuran and formula III intermediate and paraformaldehyde as raw materials, the reaction to give the intermediate of formula IV; benzyl intermediates of formula IV shown off, to give a net englitazone. The present invention is first prepared to give 1-p-chlorophenyl-2,3,4,6-tetra -O- benzyl -D- glucopyranose, then the intermediate, (S) -3- phenoxy tetrahydrofuran and paraformaldehyde as starting material to obtain net englitazone benzyl protected intermediate, the final removal of the benzyl protecting group, to give a net englitazone. Scheme present invention is shorter, a higher overall yield.
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