Application of 2-Fluorophenylacetic Acid in Drug Synthesis

Background and overview of 2-Fluorophenylacetic acid

The Chinese alias of 2-Fluorophenylacetic acid is o-fluorophenylacetic acid, which is a white to off-white shiny crystal or crystal. 2-Fluorophenylacetic acid can be used as an intermediate in pharmaceutical and chemical synthesis. If 2-Fluorophenylacetic acid is inhaled, move the patient to fresh air. If the skin comes in contact with it, you should remove the contaminated clothes and wash your skin thoroughly with soap and water. If you feel unwell, go to the hospital in time.

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Application of 2-Fluorophenylacetic acid

2-Fluorophenylacetic acid can be used as a pharmaceutical intermediate, mainly for the synthesis of prasugrel. Prasugrel is a platelet adenosine diphosphate receptor blocker. The indications are heart failure, stroke, unstable angina and other cardiovascular and cerebrovascular diseases.

2-Fluorophenylacetic acid, PCl3, NH(CH3OCH3) are used as raw materials to synthesize 2-(2-fluorophenyl)-N-methoxy-2-(methoxymethoxy)-N-methyl by one-pot method Acetamide or 2-(2-fluorophenyl)-N-methoxy-N-methylacetamide, and then react directly with Grignard reagent cyclopropylmagnesium bromide to obtain the target product 1-cyclopropyl-2 -(2-Fluorophenyl)-2-(methoxymethoxy)ethanone or 1-cyclopropyl-2-(2-fluorophenyl)ethanone. This solves the problem that phosphoramidites are unstable and difficult to prepare in the prior art, greatly simplifies the reaction, and shortens the reaction period. At the same time, the raw materials and reagents used are cheap and easily available, low cost, single product, simple post-treatment process, and high yield, which creates good conditions for industrialized large-scale production and commercialization of products.

2-Fluorophenylacetic acid is used in the preparation of 2-halo-2-(2-fluorophenyl)-1-cyclopropylethanone using low-priced phosphorus pentachloride, copper bromide, ferric chloride, etc. as halogenating reagents. In this way, the cost is reduced and there is less environmental pollution.