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Process for the peparation of 3-acylamino-4-alkoxy-phenyl-beta-hydroxysulfones and -sulfone - sulfuric acid esters

机译:制备3-乙酰氨基-4-烷氧基-苯基-β-羟基砜和-砜-硫酸酯的方法

摘要

Process for the preparation of 3- (acyl) amino-4-alkoxy-phenyl-β-hydroxyethylsulfone (sulfuric acid esters) of the formula (1) IMAGE in which R1 is alkyl of 1-4 C atoms, R2 is hydrogen or one of the groupings IMAGE, with the proviso that n = 1 when R2 = H and n = 0 when R2 = acyl by using 2-alkoxyacylanilines of the formula (2) IMAGE wherein R1 and R2 are the have the meanings mentioned, in a known manner to the corresponding sulfochlorides substituted in the p-position to the alkoxy group, the latter with alkali metal or ammonium sulfite in aqueous medium at pH 7.0-8.5 and at -5 to + 40 ° C. to the corresponding Reduced sulfinates, these alkoxylated with ethyl oxide in aqueous medium at pH 6.0-8.5 and 40-80 ° C. to give the 3- (acyl) amino-4-alkoxyphenyl-β-hydroxyethyl sulfones of the formula (1) (with R2 = Acyl and n = O) and these, if appropriate, are esterified with conc. Sulfuric acid at 70-150 ° C to the compounds of formula (1) (with R2 = H and n = 1).
机译:式(1)的3-(酰基)氨基-4-烷氧基-苯基-β-羟乙基砜(硫酸酯)的制备方法,其中R1为1-4个碳原子的烷基,R2为氢或分组之一,条件是通过使用式(2)的2-烷氧基酰基苯胺,当R2 = H时n = 1,当R2 =酰基时n = 0,其中R1和R2为提及的含义,以已知方式在对位烷氧基的对位取代的磺酰氯,后者在pH 7.0-8.5和-5至+ 40°C的水性介质中被碱金属或亚硫酸铵所取代相应的还原亚磺酸盐,它们在水介质中于pH 6.0-8.5和40-80°C下用环氧乙烷烷氧基化,得到式(1)的3-(酰基)氨基-4-烷氧基苯基-β-羟乙基砜R 2 =酰基,n = O),如果合适,将它们用浓酯化。在70-150°C的条件下将硫酸制得式(1)的化合物(R2 = H,n = 1)。

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