Li Deng-ke
2012
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Journal
Chinese Journal of Synthetic Chemistry
Abstract
7-Chloro-5-oxo-2,3,4,5-tetrahydro-1H-1-benzazepine(2) was prepared by a five-step reaction from methyl 2-amino-5-chlorobenzoate.Two key intermediates,4a and 4b,was prepared by N-acetylation of 2 with 5-nitrylpyridine-2-carbamoyl chloride or p-nitrylbenzoyl chlorid,then reduction in the presence of SnCl2.Fifteen novel potential inhibition of the AVP-V2 receptors,tolvaptan derivatives(5a~5k,6b,6i,7b and 8d) were synthesized by introducing substituted-benzoyl or substituted-phenyl-sulfonyl at amino of 4.The structures were characterized by 1H NMR,IR and MS.The SD rats diuretic test showed that some of them exhibited better diuretic activities.