159209-97-9Relevant academic research and scientific papers
Synthesis of novel D-ring fused 7′-aryl-androstano[17,16-d][1,2,4] triazolo[1,5-a]pyrimidines
Huang, Li-Hua,Zheng, Yong-Fei,Song, Chuan-Jun,Wang, Yan-Guang,Xie, Zhi-Yu,Lai, Yao-Wen,Lu, Yong-Zheng,Liu, Hong-Min
experimental part, p. 367 - 374 (2012/05/05)
The preparation of novel steroidal heterocycles containing the 7-aryl-substituted 1,2,4-triazolo[1,5-a]pyrimidine moiety fused to the 16,17-positions of the steroid nucleus is described. The Aldol reaction of 4-aza-androst-3,17-dione (1a) and dehydroepiandrosterone (DHEA, 1b) with aromatic aldehydes was catalyzed by KF/Al2O3 to give the corresponding 3-oxo-4-aza-5α- and 3β-hydroxy-5-en-16-arylidene-17- ketosteroids (2a-r). Subsequently, the intermediates 2a-r reacted with dinucleophilic 3-amino-1,2,4-triazole in presence of t-BuOK to afford the title compounds (3a-r). All the synthesized heterosteroids are new and are currently being evaluated for their biological activities.
