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Process and intermediates for the preparation of substituted 6-(3,5,6,7-tetrahydropyrrolo-2,1-c1,2,4-thiadiazol-3-ylidenimino)-7-fluoro-2H-1,4-benzoxazin-3(4H)-ones
Process and intermediates for the preparation of substituted 6-(3,5,6,7-tetrahydropyrrolo-2,1-c1,2,4-thiadiazol-3-ylidenimino)-7-fluoro-2H-1,4-benzoxazin-3(4H)-ones
The invention relates a new process for the preparation of substituted 6-(3,5,6,7-tetrahydropyrrolo[2,1-c][1,2,4]-thiadiazol-3-ylidenimino)-7-fluoro-2H-1,4-benzoxazin-3(4H)-ones of general formula I in whichR¹ is C₁-C₆-alkyl, C₂-C₆-alkenyl or C₃-C₆-alkynyl, andR² and R³, which may be the same or different, are hydrogen or C₁-C₄-alkyl,which starts from the knowna 2-amino-5-fluorophenol of formula II via the new acetanilide of formula IV in which R is hydrogen or chlorine,via the new 5-nitroacetanilide of formula V via the new 5-aminoacetanilide of formula VI via the new 5-isothiocyanatoacetanilide of formula VIII via the known benzoxazinone isothiocyanate of general formula IX and via the known iminothiadiazole of general formula XI展开▼
机译：本发明涉及一种制备取代的6-（3,5,6,7-四氢吡咯并[2,1-c] [1,2,4]-噻二唑-3-亚苄基氨基）-7-氟-2H的新方法-1,4-苯并恶嗪-3（4H）-通式I <图像文件=“ IMGA0001.GIF” he =“ 58” id =“ ia01” imgContent =“ chem” imgFormat =“ GIF” wi =“ 116” /> 在其中R 1是C 1 -C 4烷基，C 2 -C 4链烯基或C 1 -C 4炔基，和R 2和R 3可以相同或不同，是氢或C 1 -C 4烷基，从已知开始式II的2-氨基-5-氟苯酚 <图像文件=“ IMGA0002.GIF” he =“ 33” id =“ ia02” imgContent =“ chem” imgFormat =“ GIF” wi =“ 101” /> 通过新的式Ⅳ乙酰苯胺 <图像文件=“ IMGA0003.GIF” he =“ 36” id =“ ia03” imgContent =“ chem” imgFormat =“ GIF” wi =“ 113” /> 其中R是氢或氯，通过新的具有化学式V的5-硝基乙酰苯胺<化学文件ID =“ chema04”> <图像文件=“ IMGA0004.GIF” he =“ 34” id =“ ia04” imgContent =“ chem” imgFormat =“ GIF” wi =“ 110 “ /> 通过新的式VI 5-氨基乙酰苯胺 <图像文件=“ IMGA0005.GIF” he =“ 35” id =“ ia05” imgContent =“ chem” imgFormat =“ GIF” wi =“ 121” /> 通过式VIII的新的5-异硫氰酸根合乙酰苯胺 <图像文件=“ IMGA0006.GIF” he =“ 36” id =“ ia06” imgContent =“ chem” imgFormat =“ GIF” wi =“ 132” /> 通过已知的通式IX的苯并恶嗪酮异硫氰酸酯 <图像文件=“ IMGA0007.GIF” he =“ 35” id =“ ia07” imgContent =“ chem” imgFormat =“ GIF” wi =“ 116” /> 并通过已知的通式XI的亚氨基噻二唑 <图像文件=“ IMGA0008.GIF” he =“ 59” id =“ ia08” imgContent =“ chem” imgFormat =“ GIF” wi =“ 119” />
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