| 摘要 |
FIELD: chemistry. ^ SUBSTANCE: present invention relates to a method of producing montelukast of formula (I), used as a leukotriene biosynthesis inhibitor for treating asthma. The method involves the following steps: (a) reacting a halogen-phosphate compound of formula (V) with a diol compound of formula (IV) in a solvent in the presence of a base to form a phosphate compound of formula (III); and (b) mixing the phosphate compound of formula (III) with a thio-carboxylic acid of formula (II) in a solvent in the presence of a base: (I) (II) (III) (IV) (V), where R denotes H or Na; R1 denotes H, methyl or ethyl; R2 denotes methyl, ethyl or phenyl; X denotes a halogen; Y denotes sulphur or oxygen. ^ EFFECT: novel method of producing montelukast or sodium salt thereof with high degree of purity and high output. ^ 11 cl, 4 ex |
