2 results about "Wittig reaction" patented technology

This invention provides a method for preparing high-purity olaparib, belonging to the field of pharmaceutical synthesis technology. The method uses dimethyl (3-oxo-1,3-dihydroisobenzofuran-1-yl)phosphate as the starting material, reacting it with compound 2 via a Wittig reaction to generate compound 3. Compound 3 reacts with hydrazine hydrate to generate compound 4. Compound 4 is hydrolyzed and acidified to give compound 5. Compound 5 reacts with thionyl chloride to give compound 6. Compound 6 is then condensed with compounds 7 and 9 to obtain olaparib. This invention uses readily available raw materials, is simple to operate and process, has mild reaction conditions, achieves a total yield of up to 90%, a purity >99%, is environmentally friendly, and is suitable for industrial production.

The application discloses THK01 and derivatives thereof, a preparation method and application of the THK01 and the derivatives in preparation of anti-inflammatory drugs, and relates to the following steps: a series of chemical reactions, including Wittig reaction, Diels-Alder reaction, Cadogan reaction, Fischer indole synthesis reaction, demethylation reaction, reduction reaction and click chemistry reaction, are carried out on ortho-nitrobenzaldehyde containing specific substituents, so that THK01 structural modification derivatives with different substituents are obtained. The THK01 structural modification derivatives are synthesized in various routes, and the reaction success rate is high. In vitro and in vivo experiments show that the compounds can significantly inhibit the production of NO and inflammatory reactions at a low concentration, and can effectively treat inflammatory bowel disease and H1N1 virus-induced acute pneumonia in an animal model. The findings provide valuable candidate compounds and new treatment strategies for developing new, safe and efficient anti-inflammatory drugs.