Base-Promoted Reactions of Dichlorocarbene Adducts of Cyclic Enamines: A New Route to Annulated Pyrroles
作者:Alex C. Bissember、Andrew T. Phillis、Martin G. Banwell、Anthony C. Willis
DOI:10.1021/ol7021774
日期:2007.12.1
Treatment of the gem-dihalogenocyclopropanes 1-5 with potassium tert-butoxide or LDA results in the formation of the corresponding and annulated pyrroles 13-17, respectively.
用叔丁醇钾或LDA处理宝石-二卤代环丙烷1-5,分别形成相应的和环状的吡咯13-17。
Fusco,R. et al., Gazzetta Chimica Italiana, 1961, vol. 91, p. 933 - 957
作者:Fusco,R. et al.
DOI:——
日期:——
Fusco,R. et al., Gazzetta Chimica Italiana, 1961, vol. 91, p. 849 - 865
作者:Fusco,R. et al.
DOI:——
日期:——
The hit-to-lead optimization of 1,2,3,4,4a,9a-hexahydro-1H-xanthenes as glucocorticoid receptor antagonists
作者:Yan-Hui Zhu、Meng Zhang、Qun-Yi Li、Qing Liu、Jie Zhang、Yun-Yun Yuan、Fa-Jun Nan、Ming-Wei Wang
DOI:10.1016/j.cclet.2014.03.017
日期:2014.5
The structure activity relationship (SAR) study of a 1,2,3,4,4a,9a-hexahydro-1H-xanthene series of selective, human glucocorticoid receptor alpha (hGR alpha) antagonists is reported. Compounds were screened using hydroxyapatite-based GR binding and MMTV-Luc co-transfection reporter gene assays. Four different regions of the scaffold were modified to assess the effects on hGRa antagonism and related potency. Compound 8d exhibits an 8-fold better bioactivity than the original hit 1a, as well as an improved chemical stability, which make it a promising lead for the subsequent optimization. (C) 2014 Ming-Wei Wang. Published by Elsevier B.V. on behalf of Chinese Chemical Society. All rights reserved.
Migratory Aptitudes of Unsaturated Groups<sup>1</sup>