- Selective mono-amination of dichlorodiazines
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A mild, easy-to-perform, and versatile method for the formation of aminochlorodiazines from reaction of several types of dichlorodiazines (i.e., pyridazines, pyrimidines, and pyrazines) with primary or secondary amines in ethanol in the presence of trieth
- Sengmany, Stéphane,Lebre, Julie,Le Gall, Ewan,Léonel, Eric
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p. 4859 - 4867
(2015/08/03)
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- An electrochemical nickel-catalyzed arylation of 3-amino-6- chloropyridazines
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3-Amino-6-aryl- and 3-amino-6-heteroarylpyridazines have been obtained in generally good yield using a nickel-catalyzed electrochemical cross-coupling between 3-amino-6-chloropyridazines and aryl or heteroaryl halides at room temperature. Comparative experiments involving classical palladium-catalyzed reactions, such as Suzuki, Stille, or Negishi cross-couplings, reveal that the electrochemical method can constitute a reliable alternative tool for biaryl formation. A possible reaction mechanism is proposed on the basis of electrochemical analyses.
- Sengmany, Stephane,Vitu-Thiebaud, Arnaud,Le Gall, Erwan,Condon, Sylvie,Leonel, Eric,Thobie-Gautier, Christine,Pipelier, Muriel,Lebreton, Jacques,Dubreuil, Didier
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p. 370 - 379
(2013/03/13)
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- Delta 1-pyrrolines used as pesticides
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Novel Δ1-pyrrolines of the formula (I) in which R1, R2, R3, m and Q have the meanings given in the description, a plurality of processes for preparing these substances and their use for controlling pests.
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- Antihypertensives. N-1H-pyrrol-1-yl-3-pyridazinamines
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The hypothesis that the side effects of hydralazine, such as mutagenicity and lupus erythematosus like syndrome, might be due to the NHNH2 group prompted us to incorporate part of this moiety into pyrrole ring. Therefore, we prepared a series of N-1H-pyrrol-1-yl-3-pyridazinamines and a limited number of N-1H-pyrrol-1-yl-1-phthalazinamines by reaction of 3-hydrazinopyridazines and 1-hydrazinophthalazines with γ-diketones. Most of these compounds, especially in the pyridazine series, showed moderate to strong antihypertensive activity in spontaneously hypertensive rats. The decrease in blood pressure generally had a slow onset after either oral or intravenous administration. N-(2,5-Dimethyl-1H-pyrrol-1-yl)-6-(4-morpholinyl)-3-pyridazinamine hydrochloride (MDL 899) showed no mutagenic activity in several tests and is now in clinical trials in patients.
- Bellasio,Campi,Di Mola,Baldoli
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p. 1077 - 1083
(2007/10/02)
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- Cyclic alkylidenyl N-[6-(amino)-3-pyridazinyl]aminomethylenemalonates
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Compounds useful as schistosomicidal agents are cyclic alkylidenyl N-[6-(R3 R4 N)-4(or 5)-R5 -3-pyridazinyl]aminomethylenemalonates (I), where R3 R4 N is lower-tertiary-amino and R5 is hydrogen or lower-alkyl, are prepared by reacting 3-amino-6-(R3 R4 N)-4(or 5)-R5 -pyridazine (III) with cyclic alkylidenyl α-(lower-alkoxymethylene)malonate (IV) or by heating equimolar quantities of III, tri-(lower-alkyl) orthoformate and cyclic alkylidenyl malonate (V). Also shown is cyclic isopropylidenyl N-(6-methylamino-3-pyridazinyl)aminomethylenemalonate, a schistosomicidal agent, and its preparation. Also shown are schistosomicidal compositions comprising as active component a schistosomicidally effective cyclic alkylidenyl N-[6-(R3 R4 N)-4(or 5)-R5 -3-pyridazinyl]aminomethylenemalonate (I) or cyclic isopropylidenyl N-(6-methylamino-3-pyridazinyl)aminomethylenemalonate (II) or salt thereof and a method for the treatment of schistosomiasis which comprises administering to a host infected with schistosomes a schistosomicidally effective amount of said active component.
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