766497-25-0Relevant articles and documents
distress Luo river for Nepal method for preparing and its derivatives
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, (2017/03/14)
The invention discloses a preparation method of erlotinib and derivatives of erlotinib. The preparation method is characterized in that a compound II (when R2=H, the compound II is 6,7-(2-methoxyl-oxethyl)-quinoline-4-amine and a compound III (when R1=SiMe and R3=I, the compound III is 3- trimethylsilylacetylene-iodobenzene have a coupling reaction in an organic solvent under the actions of alkali, elementary substance copper and/or copper salt to obtain erlotinib and derivatives of erlotinib. The elementary substance copper and/or copper salt or palladium reagent is used as the base of the catalytic reaction, the N-(3-phenylacetylene)-6,7-di(2-methoxyl oxethyl)-4-quinoline amino acid salt (erlotinib, I) and the derivatives of erlotinib are prepared from midbody compoundS II and III. The preparation method has the advantages of use of low-price and easily available raw materials, , moderate reaction conditions, few side reaction, high yield and small environmental pollution and is applicable to the industrial production.