- Hydrogen Bond Directed Photocatalytic Hydrodefluorination and Methods of Use Thereof
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Methods of synthesizing compounds comprising fluorinated aryl groups are disclosed, wherein said methods utilize hydrogen bond directed photocatalytic hydrodefluorination.
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- PROCESS FOR PREPARATION OF HALOGENATED BENZYLAMINE AND INTERMEDIATES THEROF
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The present invention provides an improved process for the preparation of halogenated benzylamine having the formula I from halogenated benzonitriles, Formula I wherein, X1 is selected from group consisting of hydrogen, chloro or fluoro, provided atleast one X1 is chloro or fluoro.
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Page/Page column 18; 20-21
(2020/08/13)
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- Novel route for preparing dolutegravir key intermediate 2,4-difluorobenzylamine
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The invention discloses a production route which is concise and green in route, low in cost and easy to industrialize to prepare 2,4-difluorobenzylamine. The route comprises the following four steps:a) by taking m-difluorobenzene as an initial raw material, under catalysis of lewis acid, carrying out a Foucault alkylation reaction with ethylene oxide so as to prepare an intermediate 2,4-difluorobenzene ethanol; b) carrying out a second step of reactions on the product of the step a) without separation or purification, and oxidizing the 2,4-difluorobenzene ethanol to generate 2,4-difluorobenzene phenylacetic acid; c) enabling the product 2,4-difluorobenzene phenylacetic acid of the step b) with sulfoxide chloride and an ammonia gas to react so as to prepare 2,4-difluorophenylacetamide; d)under induction of bromine, enabling the product 2,4-difluorophenylacetamide of the step c) to react with a sodium hypochlorite solution, and carrying out Hofmann degradation, thereby obtaining a target product 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 and easy in industrial production.
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- 2. 4 - difluorobenzene methylamine synthetic method
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The invention relates to the fields of medicine and agrochemicals, and concretely relates to a synthetic method of an intermediate 2,4-difluorobenzene methylamine. The synthetic method comprises the following steps: 1) m-difluorobenzene, a halogenating agent and paraformaldehyde are reacted under effect of a catalyst to prepare 2,4-difluoro benzyl halide; 2)the prepared 2,4-difluoro benzyl halide and urotropine are reacted to prepare a quaternary ammonium salt compound IV; 3)the prepared quaternary ammonium salt compound is hydrolyzed by concentrated hydrochloric acid to obtain 2,4-difluorobenzene methylamine. The method has the advantages of low cost of the prepared 2,4-difluorobenzene methylamine, convenient operation and high security coefficient, and is suitable for industrial production.
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Paragraph 0044-0046
(2017/10/22)
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- Selective ruthenium-catalyzed transfer hydrogenations of nitriles to amines with 2-butanol
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Transfer your hydrogen: Fast and general transfer hydrogenation of nitriles to form primary amines is possible with a homogeneous Ru/1,4- bis(diphenylphosphino)butane (DPPB) catalyst (see scheme). The use of 2-butanol as the hydrogen-transfer reagent is essential for the selective reduction of aromatic, heteroaromatic, and aliphatic nitriles with this system. Copyright
- Werkmeister, Svenja,Bornschein, Christoph,Junge, Kathrin,Beller, Matthias
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supporting information
p. 4437 - 4440
(2013/04/23)
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- SUBSTITUTED QUINAZOLINE DERIVATIVES AND THEIR USE AS INHIBITORS
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The use of a compound of formula (I) 1 or a salt, ester or amide thereof; where X is O, or S, S(O) or S(O)2, or NR6 where R6 is hydrogen or C1-6 alkyl,; R5 is an optionally substituted 5-membered heteroaromatic ring, R1, R2 ,R3, R4 are independently selected from various specified moieties, in the preparation of a medicament for use in the inhibition of aurora 2 kinase. Certain compounds are novel and these, together with pharmaceutical compositions containing them are also described and claimed
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- 2-aminopyridine derivatives and combinatorial libraries thereof
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The present invention relates to novel 2-aminopyridine derivative compounds of the following formula: wherein R1to R5have the meanings provided herein. The invention further relates to combinatorial libraries containing two or more such compounds, as well as methods of preparing 2-aminopyridine derivative compounds.
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