The invention discloses a synthesis method of 2-substituted-3, 4-dihyidro-1-
isoquinoline ketone compound and a relative application in the
drug preparation for cardiovascular
disease, wherein the compound is represented as above, R1 is gaseous normal
alkyl and aromatic group or various substituted
alkyl and aromatic group of C1-C19, R2 is OH, OCH3, CH3, NO2 and
halogen or the like and can be one or more substituents. The preparation of 2-substituted-3, 4-dihyidro-1-
isoquinoline ketone compound uses isovanillic acid ester as
raw material, via six-step reaction as allyl etherified,
Claisen rearrangement, oxidation, reaction with primary amine (generating
Schiff base), reduction and
aminolysis of molecular
lactone, to synthesize the product. The isolated arterial ring tension test proves that the compound can relax vessel effectively. The 2-substituted-3, 4-dihyidro-1-
isoquinoline ketone compound is a new potential
cardiovascular drug, with wide application for preparing the
drug of cardiovascular
disease.