85118-02-1Relevant articles and documents
Novel method for synthesizing dolutegravir key intermediate 2,4-difluorobenzylamine
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Paragraph 0030; 0031; 0033; 0036, (2018/11/22)
The invention discloses a novel production method which is concise and green in route, low in cost and easy to industrialize to prepare 2,4-difluorobenzylamine. The method comprises the following twosteps: a) at certain pressure, carrying out a carbonylation reaction on m-difluorobenzene and CO in the presence of a catalyst so as to generate 2,4-difluorobenzaldehyde, or carrying out a formylationreaction on m-difluorobenzene, namely carrying out chlorocarbene substitution on m-difluorobenzene in a chloroform strong base system, and further carrying out hydrolysis so as to prepare a product 2,4-difluorobenzaldehyde (Reimer-Tiemann reactions); b) putting the product 2,4-difluorobenzaldehyde of the step a) into an alcohol solvent, at certain pressure, in the presence of the catalyst, carrying out a reduction ammonolysis reaction on the component with an ammonia gas and hydrogen directly in the presence of a catalyst, or enabling the component to react with ammonium formate, thereby obtaining the 2,4-difluorobenzylamine. The preparation method disclosed by the invention is simple and easy in raw material obtaining, concise in route, green and environmentally friendly, low in cost andeasy in industrial production.
A 4, 6 - double-halogenated isophthalonitrile preparation method (by machine translation)
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Paragraph 0102; 0103; 0134; 0135, (2017/07/21)
The present invention relates to the technical field of the synthesis of pharmaceutical intermediates, in particular to a 4, 6 - double-halogenated isophthalonitrile preparation method, through the use of cheap and easily obtained 2, 4 - double-halo benzoic acid as the raw material, the reaction of the halide, the amidation reaction, dehydration reaction, the nitration reaction, reduction reaction, the diazotization reaction, the substitution reaction for the synthesis of 4, 6 - double-halogenated isophthalonitrile; the total yield can be 21.5%. The process route is easily obtained and cheap materials, few by-products, the purification treatment is the process is simple, easy to realize industrial production. (by machine translation)