| 摘要 |
<p>PURPOSE: A method for preparing amlodipine is provided, thereby improving yield by using pyridinium salt as an amine protecting group and allowing mass-production of amlodipine. CONSTITUTION: The method for preparing amlodipine represented by formula (1) comprises the steps of: (a) Hantzsch reaction of pyridinium salt derivatives of formula (2), amino crotonate of formula (3) and 2-chlorobenzaldehyde of formula (4) to prepare 1,4-dihydropyridine derivatives of formula (5); and (b) reacting the 1,4-dihydropyridine derivatives of formula (5) in a mixed solvent of water and organic solvent in the presence of thiol metal salts to remove pyridine group of 1,4-dihydropyridine derivatives, wherein X- is halogen anion; the thiol metal salt is represented by formula (6), R-S-M in which M is metal, and R is C1-C10 alkyl, phenyl derivatives, perfuryl, benzyl, imidazol or thiophenyl; and the amlodipine is a calcium-channel blocker which is useful for prevention and treatment of cardiovascular disease.</p> |
