Nickel-catalyzed cross-electrophile couplings of aryl fluorosulfates with vinyl chlorosilanes
作者:Jin-He Na、Hong-Jian Du、Jia-Wen Jing、Xue-Qiang Chu、Xiao-Chun Hang、Zhi-Liang Shen、Xiaocong Zhou、Haiqing Luo
DOI:10.1016/j.jcat.2024.115636
日期:2024.9
fluorosulfates with vinyl chlorosilanes by using nickel as transition metal catalyst and manganese as reductant has been achieved. The reactions proceeded smoothly at room temperature via C-O bond activation to give a series of structurally varied aryl silanes in moderate to good yields, displaying broad substrate generality and good functional group compatibility. In addition, the reaction could be subjected
Steroidal silicon side-chain analogs as potential antifertility agents
作者:Richard H. Peters、David F. Crowe、Masato Tanabe、Mitchell A. Avery、Wesley K. M. Chong
DOI:10.1021/jm00387a011
日期:1987.4
A number of silicon-substituted analogues of ethynylestradiol that exhibit modified and enhanced biological activities have been synthesized. Particularly noteworthy are a group of [(trialkylsilyl)ethynyl]estradiol analogues that exhibit high antifertility potency and markedly reduced estrogenic activity. The best compounds synthesized are 17 alpha-[(triethylsilyl)ethynyl]estradiol (5) and 17 alpha-[(tert-butyldimethylsilyl)ethynyl]estradiol (33), which show a separation of antifertility from estrogenic activity in the rat. The results of structure-activity studies indicate a good correlation between the observed biological activities and the calculated van der Waals volumes of the three variable silicon substituents.