162515-68-6Relevant articles and documents
Preparation method of montelukast sodium side chain
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Paragraph 0015; 0024-0033, (2020/12/30)
The invention discloses a preparation method of a montelukast sodium side chain, and high-quality montelukast sodium side chain 1- (mercaptomethyl) cyclopropylacetic acid (MLM) is obtained. Accordingto the process, 1-bromo-cyclopropylacetonitrile (MLM-5) is taken as a raw material and reacts with thioacetic acid under an alkaline condition to generate benzoic acid (1-acetonitrile cyclopropyl) methyl mercaptide (MLM-6), and an alkaline hydrolysis reaction is directly performed without treatment, so that the product 1-(mercaptomethyl) cyclopropylacetic acid (MLM) is obtained. The process is simple to operate, cheap in used materials, mild in reaction condition, low in wastewater ammonia nitrogen and easy to biochemically treat, and the product yield and purity are greatly improved.
Montelukast side chain intermediate and preparing method thereof
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, (2016/11/24)
The invention belongs to the field of medical chemistry, and particularly relates to a montelukast side chain intermediate and a preparing method thereof. A provided intermediate compound is 6-halogenated methyl-5,7-dioxaspiro[2,5] octane, wherein 1,1-cyclopropyl dimethyl carbinol serving as a starting material and 2-halogeno-1,1-dimethoxyethane are subjected to a transacetalation reaction under solid acid catalysis to obtain 6-halogenated methyl-5,7-dioxaspiro[2,5] octane, the intermediate is treated with organic alkali and then hydrolyzed with a water solution containing acetic acid to obtain monoacetylated protected diol. The problems that monoacetylated protected diol is poor in selectivity, and diol loss is serious are solved, the availability of the raw materials is improved, and the montelukast side chain intermediate can be synthesized economically and conveniently.
SYNTHESIS OF LEUKOTRIENE COMPOUNDS
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Page/Page column 42; 26, (2008/06/13)
The present invention relates to the synthesis of leukotriene receptor agonist compounds and to novel intermediates employed in their preparation. Leukotriene agonists are used in the treatment of asthma, as well as other conditions mediated by leukotrienes such as inflammation and allergies. A compound of particular interest is montelukast and the present invention describes an improved process for making montelukast and similar compounds.