专利汇可以提供Preparation of 1-methyl-5- p-toluoyl pyrrole-2-acetic acid专利检索,专利查询,专利分析的服务。并且PURPOSE: To prepare the titled compound useful as an analgesic and antiphlogistic agent, in high yield, by the hydrolysis and decarbonation of a novel compound.
CONSTITUTION: 1-Methylpyrrole of formula II is made to react with a compound of formula III (R
3 and R
4 are lower alkyl or together with the adjacent N atom form a heterocyclic group such as morpholino, piperidino, etc.) in the presence of a condensation agent such as phosphorus oxychloride in a solvent to obtain 1-methyl- 5-(p-toluoyl)pyrrole of formula IV, which is made to react with a compound of formula V (R
1 and R
2 are lower alkyl) in the presence of a catalyst such as rhodium acetate, in the absence of solvent or in a solvent. The novel intermediate of formula I thus obtained, e.g. [1-methyl-5-(p-toluoyl)pyrrole-2]-malonic acid dimethyl ester, is hydrolyzed and decarbonated by heating and refluxing in a solvent such as a lower alcohol in the presence of a base such as an alkali hydroxide at 50W 120°C, for 1W10hr to afford the objective compound.
COPYRIGHT: (C)1982,JPO&Japio,下面是Preparation of 1-methyl-5- p-toluoyl pyrrole-2-acetic acid专利的具体信息内容。
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