Conversion of Esters to 2-Acetoxy Esters via 2-Nosyloxy Esters
摘要:
Reaction of 2-nosyloxy esters, available in high yields from the reaction of trimethylsilyl ketene acetals with p-((nitrobenzene)sulfonyl) peroxide, with sodium acetate in DMF produces 2-acetoxy ester in good yields.
The preparation of 2-hydrazinyl esters in high optical purity from 2-sulfonyloxy esters
作者:Robert V Hoffman、Kim Hwa-Ok
DOI:10.1016/s0040-4039(00)88996-0
日期:——
chiral 2-hydroxy esters, react enantiospecifically wilh BocNHNH2 to produce optically pure 2-hydrazinyl ester derivatives in high yields. The reaction of 2-nosyloxy esters with BocNHNH2 gives 2-(Bochydrazinyl) esters, thus providing an efficient (albeit slow) method for the conversion of esters to 2-hydrazinyl ester derivatives.
[Problem]
An excellent drug for treating or preventing cardiovascular diseases, based on cGMP production enhancing action due to soluble guanylate cyclase activating action, is provided.
[Means for Solution]
It was found that imidazopyridine compounds having a carbamoyl group at the 3-position and a substituent bonded at the 8-position via an oxygen atom in an imidazo[1,2-a]pyridine skeleton exhibits a cGMP production enhancing action by a potent soluble guanylate cyclase activating action, and is useful as a drug for treating or preventing various soluble guanylate cyclase-related cardiovascular diseases, thereby completing the present invention.