- Efficient halogenation synthesis method of aryl halide
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The invention discloses an efficient halogenation synthesis method of aryl halide. The method comprises the following step: in the presence of a catalyst (sulfoxide or oxynitride), a halogenation reagent and a solvent, carrying out a halogenation reaction on an aromatic ring compound to obtain the aryl halide. According to the present invention, in the presence of a catalyst (sulfoxide or nitrogenoxide), a halogenation reagent and a solvent, the aromatic ring is subjected to an efficient halogenation reaction, such that the very useful aryl halide can be obtained with high activity and high selectivity; and by adopting the method disclosed by the invention, aryl halides can be efficiently synthesized, and the method has a wide application prospect in actual production.
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Paragraph 0197-0201
(2021/03/31)
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- N-bromosuccinimide/dibromodimethylhydantoin in aqueous base: A practical method for the bromination of activated benzoic acids
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A new bromination method employing NBS or dibromodimethylhydantoin in aqueous base is described for the synthesis of 3-bromo-2,6-dimethoxybenzoic acid (1) and other monobrominated alkoxybenzoic acids.
- Auerbach, Joseph,Weissman, Steven A.,Blacklock, Thomas J.,Angeles, Marshall R.,Hoogsteen, Karst
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p. 931 - 934
(2007/10/02)
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- Chromatographic Separation of Enantiomers and Barriers to Enantiomerization of Axially Chiral Aromatic Carboxamides
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The enantiomers (M) and (P) of a series of similar aromatic carboxamides have been, for the first time, investigated analytically and enriched preparatively by liquid chromatography on triacetylcellulose.Enantiomeric purities (7-99percent), specific rotations, and barriers to rotation about the C(sp2)-C(sp2) bond (87 - 120 kJ/mol, Table 5) were determined.These energies are discussed in terms of the size of ortho substituents and of the buttressing effects by meta substituents.
- Cuyegkeng, Maria Assunta,Mannschreck, Albrecht
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p. 803 - 810
(2007/10/02)
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- Potential Neuroleptic Agents. 2,6-Dialkoxybenzamide Derivatives with Potent Dopamine Receptor Blocking Activities
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A series of some novel N-(1-ethyl-2-pyrrolidinylmethyl)benzamides was synthesized and tested for dopamine receptor blockade in vivo by the ability to block the apomorphine syndrome in the rat.Several compounds were considerably more potent than sulpiride as dopamine receptor blockers and displayed low liability to induce extrapyramidal side effects (catalepsy) in the rat.The blockade of dopamine receptor activity in vivo was mainly confined to the levorotatory isomers having the S absolute configuration.The structure-activity relationships are discussed.
- Florvall, Lennart,Oegren, Sven-Ove
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p. 1280 - 1286
(2007/10/02)
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- 2,6-Dialkoxybenzamides, intermediates, pharamaceutical compositions and methods for treatment of psychotic disorders
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A compound of the formula, wherein R1 is an alkyl group with 1-3 carbon atoms, R2 and R3 are the same or different and each is hydrogen, chlorine or bromine; and pharmaceutically acceptable salts and optical isomers thereof; methods and intermediates for
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