- Practical synthesis of 3-amino-4,5-dimethylisoxazole from 2-methyl-2-butenenitrile and acetohydroxamic acid
-
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.
- Tellew, John E.,Leith, Leslie,Mathur, Arvind
-
-
Read Online
- NOVEL DUAL ACTION RECEPTORS ANTAGONISTS (DARA) AT THE AT1 AND ETA RECEPTORS
-
The present invention relates to new compounds of the formula [Chemical formula should be inserted here. Please see paper copy] wherein R1, R2, R3, and R31 are as specified herein. The invention also relates to a method for preparation thereof, as well as combinations of the new compounds with previously known agents. The invention also relates to the use of the above-mentioned compounds and combinations for the preparation of a medicament for treating hypertension of different kinds, alleviating organ damage of different kinds, treating or preventing diabetic nephropathy, treating endothelin and angiotensin mediated disorders, and treating prostate cancer.
- -
-
Page/Page column 263; 270; 278-279; 283; 295; 299-300; 306; 311
(2010/11/28)
-
- Discovery and synthesis of a potent sulfonamide ET(B) selective antagonist
-
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.
- Kanda, Yasuhiko,Takahashi, Tadashi,Araki, Yoshitaka,Konoike, Toshiro,Mihara, Shin-ichi,Fujimoto, Masafumi
-
p. 1875 - 1878
(2007/10/03)
-