5554-84-7Relevant articles and documents
Synthesis method of pharmaceutical intermediate aryl sulfonyl compound
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Paragraph 0033; 0034; 0035; 0036; 0037, (2016/10/08)
The invention relates to a sulfonyl compound shown as a formula (III) used as a pharmaceutical intermediate. A synthesis method comprises the following steps: reacting compound shown as a formula (I) and a compound shown as a formula (II) in an organic solvent in the presence of a catalyst, an oxidizing agent, an auxiliary agent and an acid compound; after the reaction, treating to obtain a compound shown in the formula (III), wherein R1 and R2 are independently selected from H, C1-C6 alkyl, C1-C6 alkyloxy or nitro, and X is halogen. The method creatively employs a unique novel reaction system compounding catalyst, oxidizing agent, auxiliary agent and acid compound, and selects the appropriate organic solvent, so as to greatly increase the reactivity of materials, and accelerate the reaction process. The method has the advantages of high reaction yield, and broad industrial application prospect.
Addition of Arenesulphonyl Iodides to Substituted Phenylacetylenes
Silva Correa, Carlos M. M. da,Fleming, Maria Daniela C. M.
, p. 103 - 108 (2007/10/02)
The products of the addition of toluene-p-sulphonyl iodide to substituted phenylacetylenes (and styrenes) are studied.The regiospecificity and stereoselectivity of trans addition to acetylenes is inferred from (1)H n.m.r. spectroscopy.The effect of substituents on the reactivity of substituted phenylacetylenes towards substituted beenzenesulphonyl radicals generated by photolysis of sulphonyl iodides is studied.Phenylacetylenes with electron-donating substituents react faster.Relative reactivities yield good Hammet-Brown correlations showing the electrophilic character of sulphonyl radicals towards phenylacetylenes.The selectivity of the addition (measured by ρ) of different sulphonyl radicals towards the same set of acetylenes ranges from -0.53 to -0.93 and shows a tendency to be smaller for benzenesulphonyl iodides carrying electron donating substituents.Results are discussed in terms of polar effects on the transition state and frontier molecular orbital theory.