CAS: 42122-75-8; Methyl 5-Amino-2-Chlorobenzoate

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CAS号67-56-1 甲醇 | CAS号89-54-3 5-氨基-2-氯苯甲酸 | CAS号6307-82-0 2-氯-5-硝基苯甲酸甲酯 | CAS号7439-89-6 铁粉 | CAS号144-55-8 碳酸氢钠 | CAS号2516-96-3 2-氯-5-硝基苯甲酸 | CAS号89951-56-4 5-氨基-2-氯苯甲醇 | CAS号355368-67-1 2-CHLORO-5-(5-F... | CAS号61508-36-9 methyl 2-chloro...

2-氯-5-硝基苯甲酸置于硫酸,铁粉,氯化铵体系中,用 乙醇 作为反应溶剂,化学反应生成 5-氨基-2-氯苯甲酸甲酯
参考文献:含有肟醚或肟酯部分的新型 N-苯基三嗪酮衍生物作为有前景的原卟啉原 Ix 氧化酶抑制剂的发现
标题:含有肟醚或肟酯部分的新型 N-苯基三嗪酮衍生物作为有前景的原卟啉原 Ix 氧化酶抑制剂的发现
摘要:原卟啉原 Ix 氧化酶(ppo,Ec 1.3.3.4)是发现绿色除草剂的最重要靶标之一.为了寻找具有更高除草活性的新型ppo抑制剂,基于药效基团和支架跳跃策略,设计合成了一系列含有肟醚和肟酯基团的新型n-苯基三嗪酮衍生物.生物测定结果表明,一些化合物具有除草活性;尤其是,化合物b16在37.5 G Ai/ha的浓度下对稗草,马唐,狗尾草,苘麻,反枝苋和马齿苋表现出广谱且优异的100%除草效果,与三氟咪嗪相当.烟草ppo(Nt Ppo)酶抑制测定表明,B16表现出优异的酶抑制活性,其值为32.14 Nm,与三氟咪嗪(31.33 Nm)相似.同时,化合物b16对作物(水稻,玉米,小麦,花生,大豆和棉花)的安全性高于剂量为 150 G Ai/ha 的三氟咪嗪.而且,分子对接和分子动力学模拟进一步表明b16与nt Ppo具有非常强且稳定的结合.这表明b16可以作为潜在的ppo抑制剂和除草剂候选物在田间应用.
DOI:10.1021/acs.Jafc.4C00272

专利信息

专利号:US-8129411-B2
优先权日:2005-12-30
标题:Organic compounds
发明人：EHARA TAKERU; GROSCHE PHILIPP; IRIE OSAMU; IWAKI YUKI; KANAZAWA TAKANORI; KAWAKAMI SHIMPEI; KONISHI KAZUHIDE; MOGI MUNETO; SUZUKI MASAKI; YOKOKAWA FUMIAKI
权利人:EHARA TAKERU; GROSCHE PHILIPP; IRIE OSAMU; IWAKI YUKI; KANAZAWA TAKANORI; KAWAKAMI SHIMPEI; KONISHI KAZUHIDE; MOGI MUNETO; SUZUKI MASAKI; YOKOKAWA FUMIAKI; NOVARTIS AG
摘要:The invention relates to 3,5-substituted piperidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations comprising a 3,5-substituted piperidine compound, and/or a method of treatment comprising administering a 3,5-substituted piperidine compound, a method for the manufacture of a 3,5-substituted piperidine compound, and novel intermediates and partial steps for its synthesis. n The compounds have the formula I′ n nwherein R1, R2, T, R3 and R4 are as defined in the specification.

专利号:US-8178559-B2
优先权日:2004-12-30
标 题:Organic compounds
发明人：BREITENSTEIN WERNER; EHARA TAKERU; EHRHARDT CLAUS; GROSCHE PHILIPP; HITOMI YUKO; IWAKI YUKI; KANAZAWA TAKANORI; KONISHI KAZUHIDE; MAIBAUM JUERGEN KLAUS; MASUYA KEIICHI; IWASAKI ATSUKO; OSTERMANN NILS; SUZUKI MASAKI; TOYAO ATSUSHI; YOKOKAWA FUMIAKI
权利人:BREITENSTEIN WERNER; EHARA TAKERU; EHRHARDT CLAUS; GROSCHE PHILIPP; HITOMI YUKO; IWAKI YUKI; KANAZAWA TAKANORI; KONISHI KAZUHIDE; MAIBAUM JUERGEN KLAUS; MASUYA KEIICHI; IWASAKI ATSUKO; OSTERMANN NILS; SUZUKI MASAKI; TOYAO ATSUSHI; YOKOKAWA FUMIAKI; NOVARTIS AG
摘要:3,4-substituted piperidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations comprising a 3,4-substituted piperidine compound, and/or a method of treatment comprising administering a 3,4substituted piperidine compound, a method for the manufacture of a 3,4-substituted piperidine compound, and novel intermediates and partial steps for their synthesis are disclosed. The 3,4-disubstituted piperidine compounds have the formula (I), wherein the symbols have the meanings defined in the specification.