Synthesis of 2-alkenylpyrazol-3(2H)-one derivatives under mild conditions
摘要:
The title compounds have been synthesized by a one-pot two-stage reaction of PCI,, ketone methyl-hydrazones and methyl acetoacetate. Both stages were carried out at room temperature and the corresponding 2-alkenyl-1,5-dimethylpyrazol-3(2H)-ones 5, which are an unknown series of pyrazolones, were obtained in good yields. Use of a variety of enolizable ketones has shown that the reaction always occurs with the predominance of the (E)-isomer. X-Ray structure determinations of an (E)- and a (Z)-derivative [(E)-5c.HCl and (Z)-5b] permitted the assignment of their structures. The aromaticity of these derivatives is discussed.
The present invention encompasses compounds of general formula (1)
wherein
R
1
to R
3
are defined as in claim
1
, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.
Yandovskii,V.N.; Klindukhova,T.K., Journal of Organic Chemistry USSR (English Translation), 1974, vol. 10, p. 735 - 739
作者:Yandovskii,V.N.、Klindukhova,T.K.
DOI:——
日期:——
Bis-Heterocycles. Part II. Tetrahydro-3,3'-bi(1,2,4,5-oxatriazines)
作者:Mohammed M. Abadleh、Mustafa M. El-Abadelah、Firas F. Awwadi、Monther S. Zreid
DOI:10.3987/com-18-14015
日期:——
A new set of tetrahydro-3,3'-bi(1,2,4,5-oxatriazines) 3a-e has been prepared via condensation reaction of alkanone- and cycloalkanone N-methylhydrazones with bis-nitrile oxide. Structures of the synthesized bis-heterocycles are based on IR, NMR and MS spectral data and further by single-crystal X-ray diffraction analysis for compounds 3a and 3d. Compound 3c exhibited inhibitory activity against butyrylcholinesterase (BChE) with IC50 = 1.75 x 10(-5) mu M.
BACCOLINI, GRAZIANO, J. CHEM. SOC. PERKIN TRANS. PT 1,(1989) N, C. 1053-1056
作者:BACCOLINI, GRAZIANO
DOI:——
日期:——
Cyclic Amine Compounds and Agents for Pest Control
申请人:Hamamoto Isami
公开号:US20090259046A1
公开(公告)日:2009-10-15
Agents for pest control comprising cyclic amine compounds represented by the formula (1)
or salts thereof or N-oxides thereof as an active ingredient,
wherein Cy
1
represents an unsubstituted or substituted 5-membered heterocycle or unsubstituted or substituted group represented by the formula (a) below,
wherein Y
1
and Y
2
each independently represents nitrogen or carbon and symbol * represents the bonding positions.