171596-28-4Relevant articles and documents
Highly stereoselective one-pot construction of trisubstituted tetrahydro-β-carboline-fused diketopiperazines: A synthetic route towards cialis analogues
Jida, Mouhamad,Tourwe, Dirk,Ballet, Steven
, p. 38159 - 38163 (2014/11/08)
A facile and efficient synthetic method for the stereoselective preparation of trisubstituted tetrahydro-β-carboline-fused diketopiperazine derivatives is reported. The methodology represents a one-pot four-step reaction, employing the Ugi four-component
Synthesis and evaluation of human phosphodiesterases (PDE) 5 inhibitor analogs as trypanosomal PDE inhibitors. Part 2. Tadalafil analogs
Ochiana, Stefan O.,Gustafson, Alden,Bland, Nicholas D.,Wang, Cuihua,Russo, Michael J.,Campbell, Robert K.,Pollastri, Michael P.
scheme or table, p. 2582 - 2584 (2012/05/05)
In this Letter we describe our ongoing target repurposing efforts focused on discovery of inhibitors of the essential trypanosomal phosphodiesterase TbrPDEB1. This enzyme has been implicated in virulence of Trypanosoma brucei, the causative agent of human African trypanosomiasis (HAT). We outline the synthesis and biological evaluation of analogs of tadalafil, a human PDE5 inhibitor currently utilized for treatment of erectile dysfunction, and report that these analogs are weak inhibitors of TbrPDEB1.
An efficient and general method for the stereodivergent syntheses of tadalafil-like tetracyclic compounds
Xiao, Sen,Shi, Xiao-Xin,Ni, Feng,Xing, Jing,Yan, Jing-Jing,Liu, Shi-Ling
experimental part, p. 1711 - 1716 (2010/05/19)
A clean and general DBU-catalyzed epimerization at C-12a position of the tadalafil-like tetracyclic compounds has been fully studied. In addition, by using this clean epimerization as the key step, four stereomers of 6-d 1-tadalafil were stereodivergently synthesized from, both L- and D-tryptophan methyl ester hydrochlorides and deuterated piperonal.