CAS: 3457-46-3; 1,2-Bis(4-Chlorophenyl)Ethane-1,2-Dione

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📜1-氯-4-[2-(4-氯苯基)乙炔基]苯置于六氟异丙醇,二甲基亚砜体系中,化学反应 20.0H,以85%的收率获得产物4,4'-二氯苯偶酰
参考文献:使用hfip作为牺牲氢供体和dmso作为二羟基化剂将炔烃转化为1,2-二酮
标题:使用hfip作为牺牲氢供体和dmso作为二羟基化剂将炔烃转化为1,2-二酮
摘要:已经描述了内部炔烃的无金属和高价碘的转化为1,2-二酮化合物.本协议的效力取决于使用hfip(1,1,1,3,3,3-六氟-2-丙醇)作为炔烃的还原剂,而dmso作为烯烃的二羟基化剂来获得所需的化学转化.将获得的1,2-二酮进一步转化为有用的衍生物.
DOI:10.1016/j.Tetlet.2019.151588

专利信息

专利号:US-4286091-A
优先权日:1980-05-19
标 题:Synthesis of pyridazinone pharmaceutical intermediates using diketene reactant
发明人：BIMBER RUSSELL M; BUCHMAN RUSSELL; DEPOMPEI MICHAEL F; POWERS LARRY J
权利人:DIAMOND SHAMROCK CORP
摘要:Valuable pyridazinone intermediates to pharmaceutically useful compounds can be prepared in surprisingly high yields by the reaction of the corresponding monohydrazone with diketene, preferably in the presence of a basic catalyst. In an especially preferred embodiment, p,p'-dichlorobenzil monohydrazone and diketene are reacted in a xylene solvent in the presence of triethylamine to afford 4-acetyl-5,6-bis(p-chlorophenyl)-2H-pyridazin-3-one, which can then be reacted with ethylene carbonate in the presence of potassium carbonate to afford the antihypertensive agent, 4-acetyl-5,6-bis(p-chlorophenyl)-2-(2'-hydroxyethyl)-2H-pyridazine-3-one.

专利号:US-4281125-A
优先权日:1980-05-15
标题:Quinoline catalyzed synthesis of pyridazinone pharmaceutical intermediates
发明人：DEPOMPEI MICHAEL F; HLYNSKY ALEX
权利人:DIAMOND SHAMROCK CORP
摘要:Valuable pyridazinone intermediates to pharmaceutically useful compounds can be prepared in surprisingly high yields by the quinoline catalyzed reaction of the corresponding monohydrazone with an appropriately substituted acetic acid ester. In an especially preferred embodiment, p,p'-dichlorobenzil monohydrazone and methyl acetoacetate are reacted in a xylene solvent in the presence of quinoline to afford 4-acetyl-5,6-bis(p-chlorophenyl)-2H-pyridazin-3-one, which can then be reacted with ethylene carbonate in the presence of potassium carbonate to afford the antihypertensive agent, 4-acetyl-5,6-bis(p-chlorophenyl)-2-(2'-hydroxyethyl)-2H-pyridazin-3-one.