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2-苯基苯甲酸与对氨基苯甲酸经酰胺化反应得到4-(2-苯基苯甲酰胺基)苯甲酸(12)。同时,氨茴酸甲酯(2)经磺酰化、N-烷基化、分子内缩合关环、酸性条件下脱氰基和溴代得到1-对甲苯磺酰基-4-溴-2,3,4,5-四氢-5-氧代-1H-苯并氮,再与盐酸乙脒缩合并关环形成咪唑环、脱磺酰基得到2-甲基-1,4,5,6-四氢咪唑[4,5-d][1]苯并氮,最后与12通过酰胺化、成盐制得精氨酸加压素拮抗药盐酸考尼伐坦,总收率为25.5%(以2计)。
Amidation of 2-phenylbenzoic acid with p-aminobenzoic acid gives 4- (2-phenylbenzamido) benzoic acid (12). Meanwhile, methyl anthranilate (2) is sulfonylated, N-alkylated and condensed within the molecule. Cyano and bromo under acidic conditions give 1-tosyl-4-bromo- 3,4,5-tetrahydro-5-oxo-1H-benzazepin followed by condensation with acetamidine hydrochloride and ring closure to form an imidazole ring, desulfonylation gives 2-methyl-1,4,5,6 - tetrahydroimidazo [4,5-d] [1] benzazepin, finally with amidation and salt formation of 12, arginine vasopressin antagonist memantine hydrochloride, with a total yield of 25.5% (2).