取代-1,3-二氢吲哚-2-酮化合物的合成

Synthsis of Substituted 1,3-Dihydroindolin-2-ones

取代苯胺经酰化、环合反应制得关键中间体取代靛红衍生物4a～4k,再用三乙基硅烷/三氟乙酸体系室温还原制得取代-1,3-二氢吲哚-2-酮类化合物1a～1k,后者可用于合成舒尼替尼等酪氨酸激酶抑制剂类抗肿瘤药。

The substituted 1,3-dihydroindo-2-one compounds 1a - 1k, the intermediates of tyrosine kinase inhibitors such as sunitinib, were synthesized from substituted anilines by acylation and cyclization to give substituted isatin derivatives 4a - 4k, followed by reduction with triethylsilane/trifluoroacetic acid.