Preparing montelukast sodium, useful e.g. to antagonize leukotriene, comprises reacting sodium alkoxide compound with montelukast acid in organic solvent, where the montelukast acid is obtained by acidifying montelukast cyclohexylamine

摘要

Preparation of montelukast sodium (I), comprises reaction of a sodium alkoxide compound with montelukast acid in an organic solvent (a1), where the montelukast acid is obtained by acidification of montelukast cyclohexylamine. Independent claims are included for intermediate compounds, which are {1-[(4,4-dimethyl-4,5-dihydro-1,3-oxazol-2-yl)methyl]cyclopropyl}methane thiol (B), 2-{(R)-3-{3-[(E)-2-(7-chloro-quinol in-2-yl)-vinyl]-phenyl}-3-[1-(4,4-dimethyl-4,5-dihydro-oxazol-2-ylmethyl)-cyclopropylmethylsulfanyl]-propyl}-benzoic acid methyl ester (III), 2-(2-{(R)-3-{3-[(E)-2-(7-chloro-quinolin-2-yl)-vinyl]-phenyl}-3-[1-(4,4-dimethyl-4,5-dihydro-oxazol-2-ylmethyl)-cyclopropylmethylsulfanyl]-propyl}-phenyl)-propan-2-ol (IV), and cyclohexyl-trimethyl-ammonium (1-{(R)-1-{3-[(E)-2-(7-chloro-quinolin-2-yl)-vinyl]-phenyl}-3-[2-(1-hydroxy-1-methyl-ethyl)-phenyl]-propylsulfanylmethyl}-cyclopropyl)-acetic acid anion (V). ACTIVITY : None given. MECHANISM OF ACTION : Leukotriene antagonist; Leukotriene biosynthesis inhibitor.