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    • 32. 发明申请
    • Process for the preparation of tetrahydrothieno [3,2-C] pyridine derivatives
    • 四氢噻吩并[3,2-C]吡啶衍生物的制备方法
    • US20050137401A1
    • 2005-06-23
    • US10774506
    • 2004-02-10
    • Robert SmyjGamini Weeratunga
    • Robert SmyjGamini Weeratunga
    • C07D495/04C07D498/02
    • C07D495/04
    • A process for the preparation of tetrahydrothieno[3,2-c]pyridine compound of formula 6: or their pharmaceutically acceptable salts, wherein the meaning of X is carboxyl, alkoxycarbonyl, aryloxycarbonyl, or carbamoyl of formula wherein R1 and R2 can be individually or simultaneously hydrogen, alkyl or part of a heterocyclic structure; Z can be hydrogen, halogen, alkyl, aryl, aryloxy or alkoxy group, the process comprising conducting a dehydroxylation reaction on the compound of formula 5 in order to obtain a compound of formula 6, wherein said dehydroxylation reaction is effected by iodosilane represented by the formula Si(R3)3I, wherein R3 selected from an alkyl, alkenyl, alkynyl, aromatic group, or combinations of thereof.
    • 制备式6的四氢噻吩并[3,2-c]吡啶化合物或其药学上可接受的盐的方法,其中X的含义是羧基,烷氧基羰基,芳氧基羰基或下式的氨基甲酰基,其中R 1, SUB和R 2可以单独或同时地氢,烷基或部分杂环结构; Z可以是氢,卤素,烷基,芳基,芳氧基或烷氧基,该方法包括对式5化合物进行脱羟基化反应,以获得式6化合物,其中所述脱羟基化反应是由 其中R 3选自烷基,烯基,炔基,芳族基团或其组合,其中R 3选自烷基,烯基,炔基,芳族基团或其组合。