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Novel antipyretic and analgesic drug as well as preparation method and application thereof

An antipyretic and analgesic drug technology, which is applied in the field of new antipyretic and analgesic drugs and their preparation methods and uses, can solve the problems of lower ulcer rate, achieve high cure rate, high bioavailability, and low toxicity

Pending Publication Date: 2020-09-08
HC SYNTHETIC PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Problems: (1) The curative effect did not increase, (2) The adverse reactions did not decrease; (3) The ulcer rate decreased in the short term, and there was no difference in long-term use; (4) Severe myocardial infarction occurred

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0057] Embodiment 1: the preparation of compound 1

[0058] Take (S)-2-(3-fluoro-4-(((1S,4S)-4-fluoro-2-hydroxycyclopentyl)methyl)phenyl)propionic acid 10g, sulfuric acid 0.35g, glycine and 100ml , heated to reflux for 6 hours, evaporated to dryness under reduced pressure after the reaction was completed, and the residue was separated by chromatography to obtain 11.2 g of compound 1.

Embodiment 2

[0059] Embodiment 2: the preparation of compound 2

[0060]Take (S)-2-(3-fluoro-4-(((1S,4S)-4-fluoro-2-hydroxycyclopentyl)methyl)phenyl)propanoic acid 10g, sulfuric acid 0.3g, absolute ethanol 50ml, heated to reflux for 6 hours, evaporated to dryness under reduced pressure after the reaction was completed, 100ml of acetic acid was added to the residue, heated to reflux for 6 hours, evaporated to dryness under reduced pressure after the reaction was completed, and the residue was separated by chromatography to obtain 9.4g of compound 2.

Embodiment 3

[0061] Embodiment 3: the preparation of compound 3

[0062] Take 10g of compound 1, add 50ml of acetonitrile, cool down to 0-5°C for reaction, slowly add 6.0g of phosphorus oxychloride dropwise, react for 8 hours at 0-5°C, add 10ml of water for hydrolysis, the hydrolysis is complete, evaporate to dryness under reduced pressure, and the residual The material was separated by chromatography to obtain 12.1 g of compound 1.

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PUM

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Abstract

The invention provides an antipyretic and analgesic drug. Or a stereoisomer, hydrate, deuterated substance, ester, solvate, crystal form, metabolite, pharmaceutically acceptable salt or prodrug thereof; the structure of the antipyretic and analgesic drug is shown as a formula I. The antipyretic and analgesic drug, or stereoisomers, hydrates, deuterated substances, esters, solvates, crystal forms,metabolites, pharmaceutically acceptable salts or prodrugs thereof, has stronger clinical advantages and smaller toxicity, and is more suitable for antipyretic and analgesic treatment.

Description

technical field [0001] The invention relates to a novel antipyretic and analgesic drug as well as its preparation method and application, belonging to the technical field of medicine. Background technique [0002] Loxoprofen Sodium (Loxoprofen Sodium) is an anti-inflammatory and analgesic drug that can inhibit both cyclooxygenase COX-1 and COX-2. As the first non-steroidal anti-inflammatory drug that is the precursor of aryl propionic acid to be synthesized, the curative effect of loxoprofen sodium is mainly manifested in the significant analgesic effect, and the anti-inflammatory and antipyretic effects are comparable to other similar drugs. Clinical trials show that after oral administration, it is metabolized into a trans-OH type drug in the human body, and the concentration distribution in the liver and plasma is higher than that in other parts, and then it is quickly transformed into glucose conjugates, and finally excreted in the form of urine. The analgesic effect of...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C59/56C07C59/72C07C59/90C07C69/40C07C69/73C07C69/732C07C239/22C07F9/117A61K31/216A61K31/661A61K31/225A61K31/22A61K31/192A61P29/00
CPCC07C239/22C07C69/73C07C69/40C07C69/732C07C59/90C07C59/56C07C59/72C07F9/117A61P29/00C07C2601/08
Inventor 杨成张起愿
Owner HC SYNTHETIC PHARMA CO LTD
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