- 3,5-dichloro-4-bromoisoquinoline derivative, and preparation method and application thereof
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The invention specifically relates to a novel compound, i.e., a 3,5-dichloro-4-bromoisoquinoline derivative, and a preparation method and application thereof, belonging to the technical field of pharmaceutical synthesis. 3,5-dichloro-4-bromoisoquinoline and the derivative thereof are obtained by ring closure of 3,5-dichloro-4-bromobenzene haloethylamine through a Friedel-Crafts alkylation reaction. The 3,5-dichloro-4-bromoisoquinoline and the derivative can be used for synthesizing the important intermediate 3,5-dichloro-4-carboxylisoquinoline of Lifitegrast. According to a technical scheme in the invention, low-cost and well-supplied 2,6-dichloroaniline is used as a starting material; and the preparation method comprises a plurality steps of reactions with mild conditions, mature operation and yield of 85% or more, and each step of reaction has passed pilot-scale test, so the feasibility of industrial conversion of the method is very high and overall production cost can be greatly reduced.
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- Pesticidal compounds
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Bicyclooctane pesticides of the formula are prepared by cyclisation of In these formulae R may be various organic groups and is preferably n-butyl or n-propyl while R2 is a polysubstituted phenyl group.
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