The invention discloses a 2-(3-isoquinolinyl)-ethyl propionate derivative and a synthesis method thereof. According to the invention, O-acetyloxime with characteristics of easy preparation, structuraldiversity and multiple reaction centers is used as a raw material, the ortho-position C-H bond of the aromatic ring in the O-acetyloxime is activated under the action of a rhodium salt, a coupling reaction with allenoate is carried out, a series of 2-(3-isoquinolinyl)-ethyl propionate derivatives with different structures are synthesized, and the product can be further converted into a functionalproduct.; and the method has the advantages of easily available raw materials, simple operation, mild reaction conditions, diverse functional groups, and no need of pre-functionalization.