An efficient and practical method for large scale synthesis of (R)-6-benzyloxycarbonylamino- 1-methyl-4-(3-methylbenzyl) hexahydro-1, 4-diazepine (R-3), which is a key intermediate in the synthesis of DAT-582, a potent and selective serotonin-3 receptor antagonist, is described. The precursor of R-3, the (S)-2, 3-diaminopropylaminoacetate S-5, was obtained from the chiral triaminopropane derivative R-19. Nucleophilic reaction of the chiral ...
