公开(公告)号：US20110201792A1

公开(公告)日：2011-08-18

申请号：US13094135

申请日：2011-04-26

申请人： JENNIFER A. RIGGS-SAUTHIER ,  Nnochiri N. Ekwuribe

发明人： JENNIFER A. RIGGS-SAUTHIER ,  Nnochiri N. Ekwuribe

IPC分类号： C07C245/08

CPC分类号： C07C245/08

摘要： Methods are disclosed for preparing compounds of Formula I: where R1, R3, and R4 are independently hydrogen or C1 to C4 alkyl, and R2 is: where R5 is selected from the group consisting of hydrogen and C1 to C4 alkyl, or where R6, R7 and R8 are independently hydrogen or C1 to C4 alkyl; or the esters or pharmacologically acceptable salts thereof. The methods can involve converting a suitably functionalized aniline compound to a diazonium salt (which aniline compound can be first formed by reduction of a nitrobenzene) and coupling the diazonium salt with a suitably functionalized benzene compound. The suitably functionalized aniline compound either includes a primary alcohol or aldehyde group, which is then oxidized to a carboxylic acid group, or includes a nitrile or amide group, which is hydrolyzed to a carboxylic acid group. The methods can also involve the direct coupling (via reduction of nitro groups to form an azo linkage) of suitably functionalized nitrobenzenes. The compounds and or their metabolites can be used to treat or prevent various diseases, particularly inflammatory conditions of the GI tract.

摘要翻译： 公开了制备式I化合物的方法：其中R 1，R 3和R 4独立地为氢或C 1至C 4烷基，R 2为：其中R 5选自氢和C 1至C 4烷基，或其中R 6， R7和R8独立地是氢或C1-C4烷基; 或其酯或药理学上可接受的盐。 该方法可以包括将适当官能化的苯胺化合物转化为重氮盐（可以首先通过还原硝基苯形成苯胺化合物）并将重氮盐与适当官能化的苯化合物偶联。 适当官能化的苯胺化合物包括伯醇或醛基，然后将其氧化成羧酸基团，或包括被水解成羧酸基团的腈或酰胺基团。 所述方法还可以涉及适当官能化的硝基苯的直接偶联（通过还原硝基以形成偶氮键）。 化合物及其代谢物可用于治疗或预防各种疾病，特别是胃肠道的炎性病症。