Aedes albopictus, the main vector of dengue, yellow fever, chikungunya, and Zika, has caused significant public health concerns, but there are still few effective insecticides. Nicotine and nornicotine‐typed compounds are well‐known for their potential as an insecticide, which has potential activity against Ae. albopictus. Here we report the effects of nornicotine‐typed insecticide against larvae of Ae. albopictus. We developed a novel synthetic strategy for nicotine and nornicotine‐typed compounds. Novel compounds A1‐A8 and B1‐B26 were synthesized by the synthesized nornicotine. And bioassays indicated that most of these compounds exhibited good effects against larvae of Ae. albopictus, and compounds A3, B4, B20, and B26 had excellent activity against Ae. albopictus, and they were not toxic to humans according to other reports. After considering the cost, compounds B4, B20, and B26 could be potential lead compounds against Ae. albopictus and other Aedes mosquitoes.