Cracking catalyst and method for preparing sitafloxacin intermediate with same

Abstract

The invention discloses a cracking catalyst, which is prepared by mixing an active component with a carrier at a weight ratio of 1 to 1-3, wherein the active component is any two or more of sulfate, nitrate, halide and oxide of metal lithium, magnesium, chromium, iron, nickel, zinc, copper, aluminum, silver or palladium; the carrier is one or more of activated carbon, graphite powder and gypsum powder; the invention further discloses a method for preparing a sitafloxacin intermediate 2-chloro-2-fluoro-1-benzyloxymethylcyclopropane with the cracking catalyst; and the method comprises the following steps: step (1), filling the fully mixed catalyst into a tubular reactor equipped with a copper wire mesh, and performing nitrogen replacement treatment at 300-500 DEG C; and step (2), contactingdichlorodifluoromethane with allyl benzyl ether gas in a gas cabinet, feeding into the tubular reactor in the step (1), and continuously reacting at 500-700 DEG C to obtain the sitafloxacin intermediate 2-chloro-2-fluoro-1-benzyloxymethylcyclopropane, wherein the reaction can be carried out continuously.

Description

technical field [0001] The invention relates to a cracking catalyst and a method for preparing sitafloxacin intermediate 2-chloro-2-fluoro-1-benzyloxymethylcyclopropane by using the cracking catalyst. Background technique [0002] Sitafloxacin (Sitafloxacin) is a broad-spectrum quinolone antibacterial drug developed by Daiichi Pharmaceutical Sankyo Co., Ltd., which was first launched in Japan in 2008. It is clinically used to treat severe and refractory bacterial infections, recurrent infections and certain drug resistance Bacterial infection, has good pharmacokinetic properties, less adverse reactions, and the antibacterial activity in vitro is significantly stronger than most similar drugs. Broad antibacterial spectrum, especially strong antibacterial activity against respiratory bacteria. This product is well absorbed orally, with high bioavailability and small individual differences. After taking the drug, it is mostly excreted in the urine in the original form. Repeate...

AI Technical Summary

Problems solved by technology

Domestic and foreign studies on its synthesis mainly use diethylzinc and diiodofluoromethane to obtain fluorocarbene, and then add a series of reactions with olefins to finally obtain the target product. This route has long synthesis steps, diethylzinc is flammable and expensive , it is difficult to produce industrially

In addition, the use of ethyl diazoacetate to react with carbene and fluoroolefins under the action of a catalyst is harsh, and ethyl diazoacetate is prone to explosion during use, which also limits large-scale production