Organocatalytic annulation by functionalization of benzamide derivatives with alkynes has been developed. We report a new approach of cycloaddition under mild reaction conditions using simple catalysts, such as iodobenzene and peracetic acid, as oxidant. Those novel, mild reaction con- ditions provided a straightforward synthesis of isoquinolones with fast reaction rate. Notable selectivity in annulation of unsymmetrically disubstituted alkynes was demonstrated. CH bond functionalization has emerged over the last few decades and represents an attractive strategy to enhance molecular complexity. CH bond functionalization catalyzed by transition metals is an intensively investigated area of great significance. (1) Methods of direct coupling between non- functionalized compounds represent an environmentally benign and economically attractive synthetic strategy to the desired products. However, these methods are limited. The development of new efficient, direct oxidative cross-coupling methods is highly demanded. (1) Isoquinoline and isoquinolones represent important het- erocyclic scaffolds with broad ranges of biological activities. (2) Several attractive synthetic routes to isoquinolones were developed using transition-metal-catalyzed processes in last years. (3-8) Impressive annulation with alkynes was first devel- oped by Fagnou and co-workers employing rhodium cata- lyzed directed CH activation. (3a) Interestingly, Rovis' group independently demonstrated the annulation of benzamide with alkynes and alkenes through rhodium-catalyzed CH functionalization (Scheme 1, Eq. (1)). (4a) Recently, the Acker- mann and Wang groups reported an efficient ruthenium catalyzed approach to annulation of benzamine and alkyne (Scheme 1, Eq. (2)). (5) Very recently, palladium-catalyzed synthesis of isoquinolones has been developed by Huang and co-workers (Scheme 1, Eq. (3)). (6) Typically, transition-