13999-39-8Relevant articles and documents
Practical synthesis of 3-amino-4,5-dimethylisoxazole from 2-methyl-2-butenenitrile and acetohydroxamic acid
Tellew, John E.,Leith, Leslie,Mathur, Arvind
, p. 275 - 277 (2007)
3-Amino-4,5-dimethylisoxazole was prepared from technicalgrade 2-methyl-2-butenenitrile and acetohydroxamic acid in a 62% overall yield on a multimole scale. The key features of this synthesis are (1) DBU treatment of the technical-grade nitrile mixture to provide a starting material of acceptable purity and (2) use of acetohydroxamic acid as an N-protected hydroxylamine equivalent. This operationally simple method provides the title compound in reasonable overall yield and free of contamination from the isomeric 5-amino-3,4-dimethylisoxazole.
Discovery and synthesis of a potent sulfonamide ET(B) selective antagonist
Kanda, Yasuhiko,Takahashi, Tadashi,Araki, Yoshitaka,Konoike, Toshiro,Mihara, Shin-ichi,Fujimoto, Masafumi
, p. 1875 - 1878 (2007/10/03)
The synthesis and structure-activity relationships of a series of sulfonamide endothelin antagonists are described. In the course of our modification studies, we discovered ET(B) selective antagonists. The most potent compound 15f displays IC50 values of 1.7 μM and 0.002 μM to ET(A) and ET(B) receptors, respectively. (C) 2000 Elsevier Science Ltd. All rights reserved.