| 摘要 |
PURPOSE: A method for preparing (s)-3-amino-2,3,4,5- tetrahydro-2-oxo-1H-1-benzazepin-1-acetic acid and ester compound thereof are provided, thereby effectively and cheaply preparing the title compound under mild condition. CONSTITUTION: The method for preparing (s)-3-amino-2,3,4,5- tetrahydro-2-oxo-1H-1-benzazepin-1-acetic acid represented by formula (1) and ester compound thereof comprises the steps of: N-alkylation reacting 3-halogenated-2,3,4,5-tetrahydro-2-oxo-1H-1-benzazepin-2-one of formula (2) with halogenated acetic acid ester compound in the presence of organic solvent, base catalyst and phase transition catalyst to prepare 3-halogenated-2,3,4,5-tetrahydro-2-oxo-1H-1-benzazepine-1-acetic acid ester of formula (3); reacting the compound of formula (3) with ammonia in the presence of organic solvent to prepare 3-amino-2,3,4,5-tetrahydro-2-oxo-1H-1-benzazepine-1-acetic acid ester of formula (4); and reacting the compound of formula (4) with organic acid with enantiomeric activity to form diastereomers, wherein R is C1-C10 linear or branched, optionally saturated carbon chain, optionally saturated carbon ring, or benzene ring containing carbon chain or ring; and X is chlorine, bromine or iodine.
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