Abstract: An organic amine ester derivative drug of 2-(?-hydroxypentyl)benzoic acid and a preparation method thereof and an use thereof are disclosed. The present disclosure particularly relates to a compound having the general formula I or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable formulation prepared from the compound or the pharmaceutically acceptable salt thereof. The compound having the general formula I or the pharmaceutically acceptable salt thereof has in vitro a good solubility and a low hygroscopicity, and has in vivo a bioavailability and a brain aggregation concentration that are significantly greater than those of the original medicine butyphthalide and/or an improving drug efficacy. The use of the compound in the preparation of a drug for preventing and/or treating heart and cerebral ischemic diseases, a drug for preventing and/or treating heart and cerebral artery occlusion diseases, an anti-parkinsonian drug and an anti-senile-dementia drug is also disclosed.