A series of 5-arylamino-1,2,4-triazin-6(1H)-ones was synthesized and evaluated as antagonists at the corticotropin releasing factor receptor. Formation of CYP-mediated oxidative reactive metabolites previously observed in a related N-3-phenylpyrazinone structure was minimized by incorporation of the additional ring nitrogen found in the triazinones. (C) 2010 Elsevier Ltd. All rights reserved.
Catalytic hydrophosphorylation of alkyl- and acylhydrazones
作者:E. D. Matveeva、T. A. Podrugina、I. N. Kolesnikova、M. V. Prisyazhnoi、G. G. Karateev、N. S. Zefirov
DOI:10.1007/s11172-010-0095-2
日期:2010.2
N-Boc- and N-acylhydrazino phosphonates were obtained for the first time by hydrophosphorylation of the appropriate hydrazones of aliphatic and aromatic aldehydes and heterocyclic and aliphatic ketones in the presence of [tetra(tert-butyl)phthalocyanine]aluminum chloride as a catalyst.
作者:William D. Schmitz、Allison B. Brenner、Joanne J. Bronson、Jonathan L. Ditta、Corrine R. Griffin、Yu-Wen Li、Nicholas J. Lodge、Thaddeus F. Molski、Richard E. Olson、Xiaoliang Zhuo、John E. Macor
DOI:10.1016/j.bmcl.2010.04.121
日期:2010.6
A series of 5-arylamino-1,2,4-triazin-6(1H)-ones was synthesized and evaluated as antagonists at the corticotropin releasing factor receptor. Formation of CYP-mediated oxidative reactive metabolites previously observed in a related N-3-phenylpyrazinone structure was minimized by incorporation of the additional ring nitrogen found in the triazinones. (C) 2010 Elsevier Ltd. All rights reserved.