A new and highly potent NK1 antagonist, (aR,9R)-3 [(aR,9R)-7-[3,5-bis(trifluoromethyl)benzyl]-8,9,10,11-tetrahydro-9-methyl-5-(4-methylphenyl)-7H-[1,4]diazocino[2,1-g][1,7]naphthyridine-6,13-dione], was atropdiastereoselectively synthesized in good yield by cyclization of the chiral intermediate 6b.
Y. Ikeura, T. Doi, A. Fujishima and H. Natsugari, Chem. Commun., 1998, 2141 DOI: 10.1039/A805333B
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