Lactam compound

摘要

Disclosed is the lactam compound N-(((S)-2-hydroxy-3-methyl-butyryl)-1-(L-alaninyl))-(S)-1-amino-3-methyl-2,3,4,5-tetrahydro-2H-3-benzazepin-2-one dehydrate. Also disclosed is a process for preparing a lactam of formula I, comprising: (a) resolution of a lactam of formula (4) by crystallization as its acid addition salt, (b) coupling a compound of formula (10) with an amino-protected amino acid, to give a compound of formula (11), (c) de-protecting a compound of formula (11) to give a compound of formula (12), and (d) coupling the compound of formula (12) with a compound of formula R1CX1X2-C(O)A1, or (a2) coupling a compound of formula (1) with a compound of formula R1CX1X2-(CO)NH-CHR2-C(O)-A. The lactam compound described above is used in the manufacture of medicaments for inhibiting B-amyloid peptide release and/or its synthesis, including the treatment of Alzheimer's disease.