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📜Pyridine-2,3-Dicarboxylic Anhydride 以 丁酮 作为反应溶剂,化学反应生成 2-乙酰氨基-5-溴-6-甲基吡啶
参考文献:Pyridazinedione Compounds Useful In Treating Neurological Disorders
标题:Pyridazinedione Compounds Useful In Treating Neurological Disorders
摘要:本发明涉及吡啶并[4,5-B]喹啉及其药用盐,它们是兴奋性氨基酸拮抗剂,在需要此类拮抗作用时非常有用,例如在治疗神经系统疾病时.该发明还提供含有吡啶并[4,5-B]喹啉作为活性成分的药物组合物,以及治疗神经系统疾病的方法.

专利信息

专利号:US-8629279-B2
优先权日:2008-12-09
标 题 :Process for manufacturing 5-formyl-pyridine-2,3-dicarboxylic acid esters
发明人：RACK MICHAEL; GEBHARDT JOACHIM; MENGES FREDERIK; KEIL MICHAEL; KLIMA RODNEY F; CORTES David; LEICHT ROBERT; ZECH HELMUT; SCHROEDER JOCHEN
权利人:RACK MICHAEL; GEBHARDT JOACHIM; MENGES FREDERIK; KEIL MICHAEL; KLIMA RODNEY F; CORTES David; LEICHT ROBERT; ZECH HELMUT; SCHROEDER JOCHEN; BASF SE
摘要:A process for manufacturing a 5-formyl-pyridine-2,3-dicarboxylic acid ester (I) wherein Z is hydrogen or halogen; Z 1 is hydrogen, halogen, cyano or nitro and R 1 , R 2 are independently C 1 -C 10 -alkyl, comprising the steps of (i) reacting a compound of formula (II), wherein the symbols are as in formula (I), with a nitrosation agent (III) R 3 —O—Nâ•?O (III) wherein R 3 is C 1 -C 8 -alkyl, in the presence of an alkali metal or alkaline earth metal alcoholates or carbonates in a polar aprotic solvent at a temperature of from −45 to 40° C., to obtain an oxime compound (IV) where Z, Z 1 , R 1 and R 2 are as in formula (I), and (ii) reacting oxime compound (IV) with an aliphatic C 1 -C 10 -aldehyde in the presence of a Lewis acid at a temperature in the range of from 0 to 100° C. The compounds of formula (I) are useful intermediates in the synthesis of herbicidal imidazolinones, like imazamox.