| 摘要 |
Process for the industrial preparation of perindopril (I) and its salts by reaction of N-((S)-carbethoxy-1-butyl-(S) alanine (II) with a carbonyl derivative (III) to form a dioxo oxazolidine derivative (IV). This is reacted with an indole-2-carboxylic acid derivative (V) to form an unsaturated perindopril derivative (VI). This is hydrogenated in the presence of a catalyst to form (I). Process for the industrial preparation of perindopril (I) and its salts by reaction of N-((S)-carbethoxy-1-butyl-(S) alanine (II) with a carbonyl derivative (III) to form a dioxo oxazolidine derivative (IV). This is reacted with an indole-2-carboxylic acid derivative (V) to form an unsaturated perindopril derivative (VI). X1, X2 = leaving groups, especially Cl, imidazolyl, or trichloromethoxy; and R = H, benzyl, or 1-6C alkyl. This product is hydrogenated in the presence of a catalyst and the esterifying group is removed if necessary, to form (I). |
