The invention provides a preparation method of 5,6-dihydropyridine-2(1H)-one derivatives, specifically 1-(piperidin-2-one-1-yl)-4-(5,6-di The preparation method of hydrogen-3-R substituent pyridine-2(1H)-one-1-yl)benzene, the R substituent is chlorine or morpholin-4-yl. The present invention uses p-acetamidoaniline as a raw material, undergoes amidation with δ-valerolactone, halogenates with a halogenating agent or sulfonylates with sulfonyl chloride, condenses, deacetylates, and then reacts with 2,2-dichloro-δ - Amidation of valerolactone, halogenation with halogenating reagents or sulfonylation with sulfonyl chloride, followed by condensation elimination or condensation elimination substitution in the presence of morpholine to prepare the target product. The raw materials used in the preparation method of the invention are cheap and easy to obtain, and the cost is low; the process is simple and easy to operate, the reaction conditions are easy to realize, the amount of waste water generated is small, and it is safe and green; the reaction selectivity of each step is high, the product yield and purity are high, and it is beneficial to industrial production.