112014-73-0Relevant academic research and scientific papers
Vinyl Azides in Heterocyclic Synthesis. Part 8. Synthesis of the Naturally Occuring Phosphodiesterase Inhibitors PDE-I and PDE-II
Bolton, Richard E.,Moody, Christopher, J.,Rees, Charles W.,Tojo, Gabriel
, p. 931 - 936 (2007/10/02)
The synthesis of the naturally occuring pyrroloindole phosphodiesterase inhibitors PDE-I (1) and PDE-II (2) from isovanillin is described.The route involves the construction of both pyrrole rings by vinylnitrene cyclisations, the key cyclisation substrates being the azidoacrylates (5) and (11), prepared from the aldehydes (4) and (10) respectively.The tricyclic intermediate (12) is converted into both PDE-I and PDE-II by selective reduction, followed by carbamoylation or acetylation respectively, and deprotection.
Synthesis of the Phosphodiesterase Inhibitors PDE-I and PDE-II
Bolton, Richard E.,Moody, Christopher J.,Rees, Charles W.,Tojo, Gabriel
, p. 1775 - 1776 (2007/10/02)
The pyrroloindole phosphodiesterase inhibitors PDE-I (1) and PDE-II (2) have been synthesised from isovanilin by a route which involves construction of both pyrrole rings by thermolysis of azidoacrylates readily derived from benzaldehydes.
