CAS: 17259-32-4; 4-(6-Chloropyridazin-3-yl)Morpholine

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CAS号110-91-8 吗啉 | CAS号141-30-0 3,6-二氯哒嗪 | CAS号119-91-5 2,2'-联喹啉 | CAS号61472-02-4 N-methyl-6-morp...

📜吗啉,3,6-二氯哒嗪置于三乙胺体系中,用 异丙醇 用作溶剂,化学反应生成4-(6-氯哒嗪-3-基)吗啉
参考文献:哒嗪和哒嗪酮衍生物:其在 Lps 诱导的 Raw264.7 巨噬细胞中的抗炎潜力的合成和体外研究
标题:哒嗪和哒嗪酮衍生物:其在 Lps 诱导的 Raw264.7 巨噬细胞中的抗炎潜力的合成和体外研究
摘要:设计并合成了新的哒嗪和哒嗪酮衍生物3A-G,4A-F,6A和6B.所有化合物的细胞活力都是基于通过 Mtt 测定测定的脂多糖诱导的 Raw264.7 巨噬细胞的活力而确定的.对人 Cox-1 和 Cox-2 酶进行体外抑制测定,以探讨新合成的化合物的抗炎活性.与塞来昔布相比,最活跃的化合物 3D,3E 和 4E 对 Cox-2 的半数最大抑制浓度值分别为 0.425,0.519 和 0.356 µm.新合成的化合物抑制某些促炎细胞因子(例如诱导型一氧化氮合酶,肿瘤坏死因子-α,白介素-6 和前列腺素-E2)产生的能力也在脂多糖诱导的巨噬细胞(raw264.7 细胞)中进行了评估. ).化合物 3D 和 3E 被确定为最有效的细胞因子产生抑制剂.分子模型研究的结果表明,与参考配体相比,这些化合物的特点是对 Cox-2 活性位点具有合理的结合亲和力.在进一步研究新型抗炎药时可能会考虑这些结果.
Doi:10.1002/ddr.22173

专利信息

专利号:WO-0107416-A1
优先权日:1999-07-28
标题 :Method of producing pyridazine carboxylic acid derivatives
发明人：BESSARD YVES; CRETTAZ ROGER; EGGEL MICHAEL
权利人:LONZA AG; BESSARD YVES; CRETTAZ ROGER; EGGEL MICHAEL
摘要:The invention relates to a method of producing pyridazine carboxylic acid derivatives of the general formulae (Ia) or (Ib), wherein R<1> represents a group of the formula -OR<3> or -NR<4>R<5>, R<2> represents hydrogen, chlorine, a group of the formula -OR<6> or a group of the formula -NR<7>R<8>, R<3> represents C1-10 alkyl, C3-8 cycloalkyl or aryl-C1-4-alkyl, R<4> represents C1-10 alkyl, C3-8 cycloalkyl, optionally substituted aryl or aryl-C1-4-alkyl, R<5> represents hydrogen, C1-10 alkyl, C3-8 cycloalkyl, optionally substituted aryl or aryl-C1-4-alkyl and R<6> represents C1-10 alkyl, C3-8 cycloalkyl, aryl-C1-4-alkyl or an optionally substituted aromatic or heteroaromatic rest and R<7> and R<8> represent independently C1-10 alkyl, C3-8 cycloalkyl or aryl-C1-4-alkyl or together with the nitrogen atom form a saturated or aromatic heterocyclic ring. The inventive derivatives are obtained by reacting the corresponding 3-chloropyridazines or 3,6-dichloropyridazine with carbon monoxide and alcohols or amines H-R<1> in the presence of palladium-phosphin complexes and bases. The pyridazine carboxylic acid derivatives (Ia, Ib) are the intermediates for the synthesis of pharmaceutically active substances.