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Production manner null of nitrogen content aromatic hetero ring chemical compound

机译:氮含量芳族杂环化合物的生产方式无效

摘要

PURPOSE: To provide a new method for preparing the carboxamide of nitrogen- containing heterocyclic compound(N-heterocyclic compound) useful as an important intermediate for producing pharmaceuticals, which can be employed on an industrial scale. ;CONSTITUTION: The objective carboxamide of N-heterocyclic compound is obtained by reacting a N-heterocyclic compound with 3-35 moles, preferably 5-8 moles of formamide per mole of the N-heteroeyclic compound, in the presence of 1.1-3.0 moles of oxodisulfuric acid or its salt(preferably, ammonium salt) per mole of the N-heterocyclic compound at 20-80°C, preferably 65-75°C. It is preferable to carry out the reaction mentioned above in the presence of a strong acid in order to improve the selectivity in the carbamoylation. The carboxamide thus obtained is easily converted into a carboxylic acid of N- heterocyclic compound by hydrolysis.;COPYRIGHT: (C)1994,JPO
机译:目的:提供一种新的制备含氮杂环化合物(N-杂环化合物)羧酰胺的方法,该化合物可用作生产药物的重要中间体,可在工业规模上使用。组成:N-杂环化合物的目标羧酰胺是通过在1.1-3.0摩尔的存在下,使N-杂环化合物与3-35摩尔,优选5-8摩尔甲酰胺/摩尔的N-杂环化合物反应得到的在20-80℃,优选65-75℃下,每摩尔N-杂环化合物含氧二硫酸或其盐(优选铵盐)。为了提高氨甲酰化反应的选择性,优选在强酸的存在下进行上述反应。如此获得的羧酰胺容易通过水解转化为N-杂环化合物的羧酸。版权所有:(C)1994,日本特许厅

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