Asymmetric synthesis of (R)-6-amino-1-methyl-4-(3-methyl- benzyl)hexahydro-1H-1,4-diazepine from L-asparagine

Article abstract of DOI:10.1002/jhet.5570340516

An efficient asymmetric synthesis of (R)-6-amino-1-methyl-4-(3- methylbenzyl)hexahydro-1H-1,4-diazepine [(R)-2] which serves as the amine part of (R)-1, a potent and selective 5-HT₃ receptor antagonist, is described. Formation of the hexahydro-