872217-42-0Relevant articles and documents
Synthetic method of pyridine quinazoline intermediate
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, (2020/08/25)
The invention discloses a synthesis method of a pyridine quinazoline intermediate, which comprises the following steps: by using nitrobenzene as an initial raw material, carrying out a nitro reductionreaction, a benzene ring substitution reaction, an amino protection reaction, a chloromethylation reaction and a hydrazine hydrate cyclization reaction to obtain 3-amino-6-(perfluoropropane-2-yl)-3,4-dihydroquinazoline-2(1H)-ketone. The nitrobenzene is adopted as a starting material, benzene ring nitro reduction and benzene ring substitution reaction are achieved through a one-pot method, meanwhile, the nitrobenzene inhibits generation of fluorine-removed impurities in the benzene ring substitution reaction, the synthesis process is simplified, and the yield is increased. The chloromethylation reaction avoids the problems of many benzyl chloride impurities, strong smell, high risk and the like in the traditional route, enhances the yield, and implements the environment friendliness of thesynthesis technique. The method is simple in technological operation, low in raw material cost, environmentally friendly and suitable for large-scale production.
PROCESS FOR PRODUCING IMINOQUINAZOLINONE DERIVATIVE
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Page/Page column 11, (2010/02/15)
A novel and economical process for producing an iminoquinazolinone derivative useful as a starting material or active ingredient for medicines and agricultural chemicals. An aniline derivative represented by the general formula (II) is reacted with a halogenated formic ester to obtain a phenylcarbamic ester. The phenylcarbamic ester is reacted with a halogenating agent in the presence of a free-radical initiator to obtain a halomethylphenylcarbamic ester. The halomethylphenylcarbamic ester is reacted with hydrazine to obtain an aminoquinazoline derivative. The aminoquinazoline derivative is reacted with an aldehyde to produce an iminoquinazolinone derivative represented by the general formula (I). By the process, an iminoquinazolinone derivative useful as a starting material or active ingredient for medicines and agricultural chemicals can be efficiently provided at low cost.
