CAS: 13194-67-7; 4-Fluoro-2-Iodo-1-Methylbenzene

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上下游产品

CAS号446-10-6 4-氟-2-硝基甲苯 | CAS号367-29-3 5-氟-2-甲基苯胺 | CAS号22062-54-0 5-氟-2-甲基苯甲醇 | CAS号22062-53-9 5-氟-2-甲基苯甲醛 | CAS号22062-55-1 5-氟-2-甲基苄氯 | CAS号70931-59-8 1-(溴甲基)-4-氟-2-碘苯

5-氟-2-甲基苯胺 反应生成4-氟-2-碘-1-甲基苯
参考文献:Potential Metabolites Of Tricyclic Neuroleptics And Their Fluorinated Analogues; 3-Hydroxy-,3-Methoxy-And 3-Fluoro-10-(4-Methylpiperazino)-10,11-Dihydrodibenzo[b,F]Thiepin
标题:Potential Metabolites Of Tricyclic Neuroleptics And Their Fluorinated Analogues; 3-Hydroxy-,3-Methoxy-And 3-Fluoro-10-(4-Methylpiperazino)-10,11-Dihydrodibenzo[b,F]Thiepin
摘要:4-甲氧基-2-(苯硫基)苯甲酸(v)经过四步转化为同系物酸ixa,后者被环化为3-甲氧基二苯并[bf]噻吩-10(11H)-酮(xa).过硫噻吩(i)的3-甲氧基衍生物iii,通过中间体xia和xiia合成,并用三溴化硼去甲基化为酚化合物ii.类似的3-氟衍生物iv是由(4-氟-2-碘苯基)乙酸(xvii)合成的,其制备过程描述了几种方法.尽管iii仅具有轻微的镇静活性,Ii在中枢抑制和痉挛效应测试中比过硫噻吩(i)更有效.3-氟衍生物iv虽然不具有神经阻滞剂的特性,但具有很强的中枢抑制作用,并且这种效果在口服后有一定延长.
Doi:10.1135/cccc19792108

专利信息

专利号:US-6852711-B2
优先权日:1998-09-11
标题:HIV protease inhibitors
发明人：BOYER JR FREDERICK EARL; DOMAGALA JOHN MICHAEL; ELLSWORTH EDMUND LEE; GAJDA CHRISTOPHER ANDREW; HAGEN SUSAN ELIZABETH; LOVDAHL MICHAEL JAMES; LUNNEY ELIZABETH ANN; MARKOSKI LARRY JAMES; PRASAD JOSYULA VENKATA NAGENDR; TAIT BRADLEY DEAN
权利人:AGOURON PHARMA
摘要:The present invention relates to novel dihydropyrones with tethered heterocycles having improved pharmacologic properties which potently inhibit the HIV aspartyl protease blocking HIV infectivity. The dihydropyrones are useful in the development of therapies for the treatment of viral infections and diseases, including AIDS. The present invention is also directed to methods of synthesis of the dihydropyrones and intermediates useful in the preparation of the final compounds.