Preparation method of nabumetone

Abstract

A preparation method of nabumetone comprises the following steps: using 6-methoxy-2- naphthaldehyde, acetone solvent and 10% of sodium hydroxide as catalytic agent, and obtaining intermediate after reacting the 6-methoxy-2- naphthaldehyde, the acetone solvent and the 10% of sodium hydroxide as catalytic agent for 4 to 6 hours under temperature of 40 to 60 DEG C; dissolving the intermediate in ethyl acetate, using raney nickelas the catalyst, accessing hydrogen, besides, conducting reaction for 5 hours under temperature of 20 to 30 DEG C and pressure of 0.1 to 4 MPa, and obtaining products after treatment of steps such as filtering and recrystallizing. The preparation method of the nabumetone solves the problems that working procedure is complex in the prior art, and high temperature and pressure are needed in the hydrogenation process, and the technical problem of demanding experimental requirement in catalyzing palladium and the like, therefore, operation is simple in the whole technology, raw materials are easy to obtain, reaction steps are few, yield is high, cost is low, and mass industrial production is available.

Description

【Technical field】 [0001] The invention specifically relates to a preparation method of a non-steroidal anti-inflammatory drug nabumetone. 【Background technique】 [0002] Nabumetone is a new type of non-acidic non-steroidal anti-inflammatory drug. Analgesic and anti-inflammatory effects, the drug is much less irritating to the stomach than indomethacin and aspirin. It is used for rheumatoid arthritis and osteoarthritis. In recent years, the domestic and foreign market demand has increased significantly year after year, and the development prospect is very optimistic. In recent years, there are many industrial preparation methods about nabumetone, mainly the following methods: [0003] Method 1 (US5750793A; EP0792860A1): [0004] [0005] The disadvantages of this method are: due to the existence of bromine, the catalytic hydrogenation temperature is high, the time is long, the pressure is high, and the catalyst recovery is difficult at the same time; the three wastes are...

AI Technical Summary

Problems solved by technology

[0005] The disadvantages of this method are: due to the presence of bromine, the catalytic hydrogenation temperature is high, the time is long, the pressure is high, and the recovery of the catalyst is difficult at the same time; the three wastes are difficult to handle; the total yield is low

[0008] The disadvantage of this method is: it is synthesized with raw materials 6-methoxy-2-naphthaldehyde and ethyl acetoacetate, the preparation process is complicated, the total yield is low, and the cost is high

[0011] The disadvantage of this method is: the total yield is about 80%, but the raw materials are expensive and not easy to obtain, so the cost is high

[0014] The disadvantages of this method are: heterogeneous solvents are used, and there is a lot of waste water; the first step of the Heck reaction requires strict nitrogen protection, and the process is complicated; the reaction also uses expensive palladium catalysts, and the cost is high

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