Pal Manojit, Dakarapu Rambabu, Padakanti Srinivas
Chemistry-Discovery Research, Dr. Reddy's Laboratories Ltd., Bollaram Road, Miyapur, Hyderabad 500049, India
J Org Chem. 2004 Apr 16;69(8):2913-6. doi: 10.1021/jo049923t.
3-Methylindole is acylated regioselectively at the methyl group when treated with a variety of acyl chlorides in 1,2-dichloroethane in the presence of AlCl(3), affording a mild and direct method for the synthesis of 3-(2-oxoalkyl)indoles. The product formation in this one-pot reaction largely depends on the conditions of the reaction employed. The methodology does not require protection-deprotection steps and is amenable for the scale-up synthesis of these indole derivatives.
当在三氯化铝存在下，于1,2 - 二氯乙烷中用多种酰氯处理时，3 - 甲基吲哚在甲基处发生区域选择性酰化反应，从而提供了一种温和且直接的合成3 -（2 - 氧代烷基）吲哚的方法。该一锅法反应中的产物形成在很大程度上取决于所采用的反应条件。该方法不需要保护 - 脱保护步骤，并且适合这些吲哚衍生物的放大合成。
