申请人:——
公开号:US20040014986A1
公开(公告)日:2004-01-22
The invention relates to a method for producing 2-oxindoles from the corresponding isatines of formula (I), wherein R can be H, CH
3
, phenyl or benzyl and R
1
can be H, C
1
-C
4
-alkyl, C
1
-C
4
-alkoxy, phenyl, phenoxy, halogen, amino, nitro or hydroxy. Said isatines are converted by means of hydrazine hydrate in a polar solvent at a temperature of 15 to 185° C. to form a corresponding isatine hydrazone which directly undergoes further reaction to form the corresponding 2-oxindole of formula (II) by adding diazabi-cyclooctane and/or diazabicycloundecane and/or ethyldiisopropylamine as a catalyst in temperatures of 100 to 185° C., whereby the produced reaction water is distilled off. According to formula (II), R and R
1
have the aforementioned definitions. The 2-oxindole is isolated from the reaction mixture by distilling off the solvent and by means of crystallisation.
1
本发明涉及一种从式(I)中对应的异喹啉制备2-氧吲哚的方法,其中R可以是H,CH3,苯基或苄基,R1可以是H,C1-C4烷基,C1-C4烷氧基,苯基,苯氧基,卤素,氨基,硝基或羟基。所述异喹啉通过在极性溶剂中以15至185℃的温度利用肼水合物转化为相应的异喹啉肼酮,直接通过在100至185℃的温度下加入咪唑环辛烷和/或咪唑双环十一烷和/或乙基二异丙基胺作为催化剂进一步反应,产生的反应水被蒸馏掉,形成相应的2-氧吲哚(II),其中R和R1具有上述定义。通过蒸馏溶剂和结晶的方法从反应混合物中分离出2-氧吲哚。