0]hept- 2-en-2-yl)oxy]-2H-1-benzopyrans and their analogues were synthesized and evaluated on potassium channel opening and hypotensive activities. Compound (-)-13B with a (4-methyl-5-oxo-3,4-diazabicyclo[4.1.0]hept-2-en-2-yl)oxy group for the 4-position of the benzopyran ring was 3 times as potent as EMD 57283 (II), the lead compound, in hypotensive activity. The results would demonstrate that 5-oxo-3,4-diazabicyclo[4
Synthesis and Modular Reactivity of Pyrazole 5-Trifluoroborates: Intermediates for the Preparation of Fully Functionalized Pyrazoles
作者:Prisca Fricero、Laurent Bialy、Andrew W. Brown、Werngard Czechtizky、María Méndez、Joseph P. A. Harrity
DOI:10.1021/acs.joc.6b02847
日期:2017.2.3
The regioselective condensation of hydrazines and ynone trifluoroborates provides access to a range of pyrazole 5-trifluoroborates. The stability of the borate unit allows chemoselective halogenation of the heteroaromatic ring, thereby delivering pyrazole scaffolds that allow orthogonal functionalization at C5 and C4. The modular reactivity of these intermediates is exemplified by cross-coupling reactions
4-AMINO-5-METHYLPYRAZOLE DERIVATIVES AND PROCESS FOR PRODUCTION THEREOF
申请人:Sankyo Agro Company, Limited
公开号:EP1580189A1
公开(公告)日:2005-09-28
The present invention relates to 4-amino-5-methylpyrazole derivatives represented by the following formula (I):
(wherein R1 represents an isobutyl group, a cyclobutylmethyl group, a neopentyl group or the like) or a salt thereof, which are novel compounds being useful as synthetic intermediates of pharmaceuticals, agricultural chemicals or the like.
Syntheses and Diels-Alder reactions of 2-alkylazo-substituted 1,3-butadienes
作者:Klaus Banert、Manfred Hagedorn
DOI:10.1016/s0040-4039(00)60179-x
日期:1992.11
1-Alkyl-1-(2,3-butadienyl)hydrazines 1b,d—g can be oxidized under mild conditions to yield 1-alkyl-2-(1-methylen-2-propenyl)diazenes 3. These E-configurated azo compounds are precursors for rapid inter- and intramolecular [4+2] cycloadditions to give the heterocyclic products 4 and 6–10.