CAS: 40750-59-2; 3,4-Dichloro-N-Methylaniline

上下游产品

2-(N-Methyl-3,4-dichloranilino)-2-methyl-2-phenylacetonitril 2-(N-Methyl-3,4-dichloranilino)-2-phenylacetonitril N-(3,4-dichlorophenyl)formamide m,p-dichloroaniline N-butyl-N'-(3,4-dichloro-phenyl)-N,N'-dimethyl-ureaN-butyl-N'-(3,4-dichloro-phenyl)-N,N'-dimethyl-urea N-methyl-N-(3,4-dichlorophenyl)carbamoyl chloride 1-(3,4-Dichloro-phenyl)-3-(2,3-dichloro-propionyl)-1-methyl-urea 3-(2,3-Dibromo-propionyl)-1-(3,4-dichloro-phenyl)-1-methyl-urea

N-(3,4-二氯-苯基)-甲酰胺置于lithium Aluminium Tetrahydride体系中,用 四氢呋喃 作为反应溶剂,以90%的收率获得产物3,4-二氯-N-甲基苯胺
参考文献:来自卡氏肺孢子虫和弓形虫的二氢叶酸还原酶的2,4-二氨基吡啶并[3,2-D]嘧啶抑制剂.
标题:来自卡氏肺孢子虫和弓形虫的二氢叶酸还原酶的2,4-二氨基吡啶并[3,2-D]嘧啶抑制剂.
摘要:由以下化合物合成了六个先前未知的2,4-二氨基-6-(苯胺基甲基)-和2,4-二氨基-6-[(n-甲基苯胺基)-甲基]吡啶基[3,2-D]嘧啶(5-10)通过在室温下在存在或不存在nahco3的条件下,用适当的苯胺或n-甲基苯胺在二甲基甲酰胺中处理,来制备2,4-二氨基-6-(溴甲基)-吡啶并[3,2-D]嘧啶氢溴酸盐(11.Hbr).测试了化合物5-10作为卡氏肺孢子虫,弓形虫和大鼠肝脏中二氢叶酸还原酶的抑制剂,这是针对发现兼具高酶选择性和高效力的亲脂性非经典抗叶酸药物的一项较大努力的一部分.在所测试的六个类似物中,对弓形虫dhfr最有效和最具选择性的是2,4-二氨基-6-[(3',4',5'-三甲氧基-N-甲基苯胺基)甲基]吡啶基[3,2-Dd嘧啶(7),Ic50为0.0047 Microm(针对该酶)与0.026 Microm(针对大鼠肝酶)相比.7对刚地弓形虫dhfr的效价与曲美
DOI:10.1021/jm00014A014

专利信息

专利号:WO-2012149093-A1
优先权日:2011-04-26
标 题 :2-guanidino-4-oxo-imidazoline derivatives as antimalarial agents, synthesis and methods of use thereof
发明人：LIN AI J; LIU XIANJUN; KOZAR MICHAEL P; O'NEIL MICHAEL T
权利人:US OF AMERICA AS REPRESENTED BY THE SECRETARY OF ARMY; LIN AI J; LIU XIANJUN; KOZAR MICHAEL P; O'NEIL MICHAEL T
摘要:The present invention relates to new 2-guanidino-4-oxo-imidazoline derivatives (deoxo-IZ), methods of making these compounds, compositions containing the same, and methods of using the same to prevent, treat, or inhibit malaria in a subject.