Title: A One-pot Method for the Synthesis of 14-O-[(2-Amino-1,1-dimethylethyl)thiomethylcarbonyl]mutilin
Abstract:Valnemulin intermediate,14-O-[(2-amino-1,1-dimethylethyl)thiomethylcarbonyl]mutilin,was prepared by one-pot method with pleuromutilin,4-toluenesulfonyl chloride and dimethylcysteamine hydrochloride in...Valnemulin intermediate,14-O-[(2-amino-1,1-dimethylethyl)thiomethylcarbonyl]mutilin,was prepared by one-pot method with pleuromutilin,4-toluenesulfonyl chloride and dimethylcysteamine hydrochloride in diethyl ether.The optimum conditions were ascertained as follows:n(pleuromutilin)∶ n(4-toluene sulfonyl chloride)∶ n(dimethyl cysteamine hydrochloride)=1∶ 1.1∶ 1.1,tetrabutyl ammonium bromide being used as phase transfer catalyst,the amount of tetrabutyl ammonium bromide being 1.6 g,reaction time 2.5 h,reaction temperature 30 ℃;under such optimum conditions,the yield of the product was 91%.An orthogonal design incorporating 4 factors at 3 levels was applied to optimize the main process conditions,the results of which were in accordance with the single factor experimental data.The structure of the target compound was characterized by means of 1HNMR,IR and its melting point was measured.Read More
Publication Year: 2012
Publication Date: 2012-01-01
Language: en
Type: article
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