33 results about "Diazoacetic ester" patented technology

The invention belongs to the field of the drug synthesis, relating to the novel synthesis method of the natural drug physostigmine preventing the disease of Alzheimer and the derivatives aniline formic ester phenserine. In the invention, the L-tryptophan 3 is used as the raw material; first the chiral oxazolone intermediate 5 is made; then through the three-step and one-pot chute-typed reaction between the molecules of the asymmetric cyproterone, opening of the ring and cyclization, the intermediate 5 reacts with the diazo acetate ester to prepare the optically pure 3-substituted tetrahydropyrrole indole skeleton 6; the skeleton is deoxidized by the tetra-lithium aluminum hydride to get the diol substituted intermediate 7; the intermediate 7 is doffed from the hydroxy-methyl by the Raney-Ni to get the intermediate 8 desoxyeseroline; the intermediate 8 finishes the synthesis of the physostigmine preventing the disease of Alzheimer and derivatives aniline formic ester phenserine, after the bromination, the methyl-etherification, the doffing of the methyl and the carbonylation reactions. The method has the advantages of the high collection rate of the key reactions, the simple operation, and the short reaction steps and so on; and the method has the important practical significance for the solution of the sources of the raw materials of the drug physostigmine and the derivatives aniline formic ester phenserine in the market.