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    • 3. 发明申请
    • PROCESS FOR PREPARING 6,7-DIHYDRO-5H-IMIDAZO[1,5-A]PYRIDIN-8-ONE
    • 制备6,7-二氢-5H-咪唑并[1,5-a]吡啶-8-酮的方法
    • WO2007113235A1
    • 2007-10-11
    • PCT/EP2007/053078
    • 2007-03-30
    • Speedel Experimenta AGMARTIN, PierreBOUDIER, AndreasQUIRMBACH, MichaelMAH, RobertJOTTERAND, Nathalie
    • MARTIN, PierreBOUDIER, AndreasQUIRMBACH, MichaelMAH, RobertJOTTERAND, Nathalie
    • C07D213/65C07D233/22C07D471/04C07F7/08C07F7/18
    • C07D233/22C07D213/65C07D471/04C07F7/0814
    • 6,7-Dihydro-5H-imidazo[1,5-a]pyridin-8-one (I), is obtainable in high yields by: 1) a process which proceeds from a suitably protected C-(3-hydroxypyridin-2-yl)methylamine whose amine is converted to the formamide which is then cyclized to the imidazo[1,5- a]pyridine and hydrogenated to the 6,7-dihydro-5H-imidazo[1,5-a]pyridin-8-one, and suitably protected C-(3-hydroxypyridin-2-yl)methylamines can be prepared either in 2 steps proceeding from commercially available 3-hydroxy-2-cyanopyridine [932-35-4] or in 3 steps proceeding from commercially available 2-hydroxymethylpyridin-3-ol [14173-30-9]; 2) a process for preparing 4-hydroxy-1-(1H-imidazol-4-yl)butan-1-one, an intermediate from the synthesis of 6,7-dihydro-5H-imidazo[1,5-a]pyridin-8-one (formula I), as described in WO 2002/040484, proceeding from N,N-dimethyl-2-(trialkylsilanyl)imidazole-1-sulphonamide by lithiation and subsequent reaction with a suitably protected 4-hydroxybutyraldehyde, followed by oxidation of the secondary alcohol, acid-induced deprotection of the imidazole and deprotection of the alcohol functionality; 3) a process which proceeds from 5,6,7,8-tetrahydroimidazo[1,5-a]pyridine [38666-30-7], which is oxidized.
    • 6,7-二氢-5H-咪唑并[1,5-a]吡啶-8-酮(I)可以通过以下方式获得:1)从适当保护的C-(3-羟基吡啶-2 - 基)甲胺,其胺转化为甲酰胺,然后将其环化为咪唑并[1,5-a]吡啶,并氢化成6,7-二氢-5H-咪唑并[1,5-a] 一种适当保护的C-(3-羟基吡啶-2-基)甲胺可以从市售的3-羟基-2-氰基吡啶[932-35-4]或以商业上可获得的3个步骤 2-羟甲基吡啶-3-醇[14173-30-9]; 2)制备4-羟基-1-(1H-咪唑-4-基)丁-1-酮的方法,由6,7-二氢-5H-咪唑并[1,5-a]吡啶 -8-(咪唑-1-基)磺酰胺的N,N-二甲基-2-(三烷基硅烷基)咪唑-1-磺酰胺进行的步骤(WO 2002/040484中所述),然后与适当保护的4-羟基丁醛反应,随后与 仲醇的氧化,酸诱导的咪唑脱保护和醇官能团的脱保护; 3)从被氧化的5,6,7,8-四氢咪唑并[1,5-a]吡啶[38666-30-7]进行的方法。