4-substituted-4-(N-propionyl) aniline piperidine compound and preparation method and application thereof

Abstract

The invention relates to a 4-substituted-4-(N-propionyl) aniline piperidine compound and a preparation method and application thereof. The structure of the compound is shown in Formula (I) or hydrochloride thereof, wherein R1 is a substituent with a mother nucleus structure of propofol, and R2 is 3-methyl propionate group or a benzyl group. The compound can be dissolved in water, and can achieve analgesic and sedative effects simultaneously. Thus, the compound is applicable to analgesia and sedation of patients needing postoperative care, and is particularly conducive to operation of the automatic dosing system by patients, and the operations by anesthesia doctors can be reduced. According to the basic preparation method, the compound is prepared via condensation of propofol (III) and a 4-formyl-4-(N-phenyl propoxy amide)-N-substituted piperidine compound (II).

Description

technical field [0001] The invention relates to a compound with general anesthesia and analgesic effects, especially 4-substituted-4-(N-propionyl)aniline piperidine compounds, a preparation method and pharmaceutical use of the compound. Background technique [0002] In the medical activities of clinical operation and postoperative monitoring, the combined use of analgesia, sedation and anesthesia drugs ensures the patient's surgical compliance. The current clinical anesthesia is monitored anesthesia under the control of doctors. Anesthesiologists need to pay attention to the patient's vital signs at any time and carry out targeted treatment of the patient's pain. The realization of these treatments mainly depends on the use of various analgesic and sedative drugs. Currently commonly used analgesic drugs are opioid agonists, such as fentanyl and remifentanil. Remifentanil (Remifentanil, 3 [4 (methoxycarbonyl) - 4- (N-phenylpropanylamino) 1-piperidine] propionate methyl este...

AI Technical Summary

Problems solved by technology

However, although propofol can produce better sedative effect when it is lower than the anesthetic concentration, it is currently used in the form of emulsion because of its low water solubility, and a large amount of fat emulsion is not suitable for the long-term treatment of postoperative patients. time administration