100134-82-5Relevant articles and documents
A Scalable Synthesis of 2-(1,2,4-Oxadiazol-3-yl)propan-2-amine Hydrobromide Using a Process Safety-Driven Protecting Group Strategy
Likhite, Nachiket,Lakshminarasimhan, Thirumalai,Rao, Mallem H. V. Ramana,Shekarappa, Vijaykumar,Sidar, Somprabha,Subramanian, Varadharajan,Fraunhoffer, Kenneth J.,Leung, Simon,Vaidyanathan, Rajappa
, p. 1328 - 1335 (2016)
A safe and scalable synthesis of 2-(1,2,4-oxadiazol-3-yl)propan-2-amine hydrobromide is described. A process safety-driven synthetic strategy was employed for the selection of thermally stable compounds en route to the target 1,2,4-oxadiazole. Application
The Synthesis of Ketone-Derived Enamides by Elimination of HCN from Cyanoamides
Coussanes, Guilhem,Gaus, Katharina,O'Sullivan, Anthony C.
, p. 4176 - 4188 (2016/08/26)
Treatment of easily available ketone-derived cyanoamides with NaOtBu leads to enamides in a simple, scalable, and inexpensive one-step operation in good yield. Enamides not stabilized by conjugation or by inclusion in a ring can also be prepared. An E1cB mechanism consistent with all results and observations, is proposed. The Z geometry of the product enamide is highly favoured, and the regioselectivity can be directed by one′s choice of protecting group.
Structural modifications of 5,6-dihydroxypyrimidines with anti-HIV activity
Guo, Di-Liang,Zhang, Xing-Jie,Wang, Rui-Rui,Zhou, Yu,Li, Zeng,Xu, Jin-Yi,Chen, Kai-Xian,Zheng, Yong-Tang,Liu, Hong
supporting information, p. 7114 - 7118 (2013/01/15)
A series of 5,6-dihydroxypyrimidine analogs were synthesized and evaluated for their anti-HIV activity in vitro. Among all of the analogs, several compounds exhibited significant anti-HIV activity, especially 1b and 1e, which showed the most potent anti-HIV activity with EC50 values of 0.14 and 0.15 μM, and TI (therapeutic index) values of >300 and >900, respectively. Further docking studies revealed that the representative compounds 1e and 3a could meet the HIV-1 integrase inhibition minimal requirements of a chelating domain (two metal ions) and an aromatic domain (π-π stacking interactions).