The invention discloses an isolongifolenone-caprolactam derivative, a preparation method and an application thereof. The present invention uses isolongifolyl caprolactam derivatives as raw materials and cinnamoyl chloride derivatives as acylating reagents to undergo an acylation reaction under the catalysis of a base to prepare 3-cinnamoyl-5,5,9,9 ‑Tetramethyl‑4, 5, 6, 7, 8, 9‑hexahydro‑5a, 8‑endomethylenebenzo[d]azepine‑2(3H)‑ketones. The application has been proved by experiments that 3-cinnamoyl-5,5,9,9-tetramethyl-4,5,6,7,8,9-hexahydro-5a, 8-endomethylene benzo[d The ]azepine-2(3H)-ketone compound has good inhibitory activity on human breast cancer cell MCF-7, and has potential application value in the preparation of anti-tumor drugs.