- Montelukast side chain intermediate and preparing method thereof
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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.
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Paragraph 0059; 0060; 0061
(2016/11/24)
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- NOVEL PROCESS FOR PREPARING 1-(MERCAPTOMETHYL) CYCLOPROPANEACETIC ACID, A USEFUL INTERMEDIATE IN THE PREPARATION OF MONTELUKAST AND SALTS THEREOF
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The present invention provides a novel montelukast intermediate and a simple and straightforward process for preparing it. According to the present invention, by using this intermediate and the process, essentially as described herein, montelukast acid and salts thereof are obtained.
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Page/Page column 8; 12
(2008/06/13)
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- Process for preparation of [1-(mercaptomethyl)cyclopropyl]acetic acid and related derivatives
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The present invention provides a novel process for preparing [1-(mercaptomethyl)cyclopropyl]acetic acid with high purity and related derivatives.
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Page/Page column 7
(2008/06/13)
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- Substituted 5-benzyl-2,4-diaminopyrimidines
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The invention relates to substituted 5-benzyl-2,4-diaminopyrimidines of general formula (A) wherein R1is C2-C3 alkyl an R2is heterocyclyl, phenyl or naphthyl, bonded by one of its C-atoms and R3is C2-C6 alkyl, alkenyl, cycloalkyl, cycloalkylalkyl, heterocyclylalkyl, alkylsulfonyl, cycloalkylsulfonyl, cycloalkylalkylsulfamoyl, heterocyclysylfonyl, heterocyclylalkylsulfonyl or dialkylsulfamoyl; wherein alkyl, cycloalkyl and alyenyl can carry up to 6 carbon atoms alone or in compositions and can carry up to 6 ring members heterocyclically, alone, or in compositions and the groups R2and R3can be substituted; and to acid addition salts of compounds. The invention also relates to a method for producing the above 5-benzyl-2,4-diaminopyrimidines, to the intermediate. products that are produced, to corresponding medicaments and to the use of 5-benzyl-2,4-diaminopyrimidines as medicinal preparations. The products have antibiotic properties and are useful for combating or preventing infectious diseases.
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Page column 48
(2010/02/09)
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