99419-61-1Relevant articles and documents
A synthesis method of erlotinib hydrochloride (by machine translation)
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Paragraph 0030; 0031;0032; 0033; 0034; 0035, (2017/06/30)
The invention relates to a technical field of drug synthesis, relates to a new synthetic method of erlotinib hydrochloride. The steps are as follows: 1) to acetophenone as a starting material, in the nitration reaction takes place in the mixed between nitro acetophenone; 2) between nitro acetophenone with chlorinated reagent in the organic solvent in the reaction of chloride 1 - chloro - 1 - (3 - nitrophenyl) ethylene; 3) 1 - chloro - 1 - (3 - nitrophenyl) ethylene in the presence of an organic solvent and alkali to obtain between the dehydrochlorination nitrobenzene acetylene; 4) m acetylene through the nitro-selective reduction to obtain between amino acetylene; reduction method as a reducing agent or catalytic hydrogenation reduction; 5) between amino acetylene and 4 - chloro - 6, 7 - b - (2 - methoxyethoxy) quinazoline in reaction of organic solvent to obtain the erlotinib hydrochloride; raw materials of the invention is cheap, low production cost, simple operation, mild reaction conditions and the like, and is suitable for industrial production. (by machine translation)