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    • 2. 发明公开
    • Process for the deprotection of N-substituted azetidones
    • Verfahren zumentschützenvon N-substitutionierten Azetidonen
    • EP1256572A1
    • 2002-11-13
    • EP01870100.3
    • 2001-05-10
    • Tessenderlo Chemie S.A.
    • Ceresiat, Marcel Maurice GhislainBelmans, MarcMarchand-Brynaert, JaquelineLaurent, Mathieu
    • C07D205/08
    • C07D205/08Y02P20/55
    • The present invention relates to a method for the preparation of a compound of the general formula (I) wherein

      R 1 and R 2 each represent independently hydrogen, halogen, hydroxy, thiol, nitro, amino, carboxy, amino derivative, oxy derivative, thio derivative, alkyl, alkenyl, alkynyl, aryl, oxy derivative, amino derivative, thiol derivative, acyl derivative, acyloxy derivative, ester, amido, ether, arylalkyl, heterocycle or Me(OR')CH wherein R' is hydrogen or R a R b R c Si wherein R a , R b and R c is independently chosen from the group consisting of alkyl, alkenyl, alkynyl, aryl or a heterocycle;
      R 3 represents a protecting group such as alkyl, alkenyl, alkynyl, or arylalkyl;
      wherein this method comprises the reaction of a compound of the general formula (II) in the presence of a halogen-radical source, water and a proton donor suitable as a catalyst.
    • 本发明涉及制备通式(I)的化合物的方法,其中R 1和R 2各自独立地代表氢,卤素,羟基,硫醇,硝基,氨基,羧基,氨基衍生物, 氧基衍生物,硫代衍生物,烷基,烯基,炔基,芳基,氧基衍生物,氨基衍生物,硫醇衍生物,酰基衍生物,酰氧基衍生物,酯,酰胺基,醚,芳基烷基,杂环或Me(OR')CH,其中R' 或R a R c R c Si,其中R a,R b和R c独立地选自烷基,烯基,炔基,芳基或杂环; R 3表示保护基如烷基,烯基,炔基或芳基烷基; 其中该方法包括通式(II)的化合物在卤素自由基源,水和适合作为催化剂的质子给体存在下的反应。