Tert-butyl 7-amino-4,5-dihydro-1H-benzo[D]azepine-3(2H)-carboxylate → 1,2,4,5-Tetrahydro-benzo[d]azepine-3-carboxylic acid tert-butyl ester

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Reaction Steps

748-(5-Chloro-2-propoxy-phenyl]-[1,2,4]triazolo[1,5a]pyridine-2-ylamino]1,2,4,5-tetrahydro-benzo[d]azepine-3-carboxylic acid tert-butyl ester was prepared from 2-chloro-8-(5-chloro-2-propoxy-phenyl)-[1,2,4]triazolo[1,5-a]pyridine and 7-amino-1,2,4,5-tetrahydro-3-benzazepin-3-carboxylic acid tert-butyl ester with 2,2′-bis-dicyclohexylphosphanyl-biphenyl as the ligand in a manner analogous to Example 2d (0.14 g, 46%). MP=127-129° C. 1H NMR (400 MHz, (D3C)2SO, δ, ppm): 9.60 (s, 1H), 8.76 (d, 1H), 7.72 (s, 1H), 7.65 (m, 1H), 7.42 (m, 3H), 7.20 (m, 1H), 7.05 (m, 2H), 3.97 (m, 2H), 3.43 (m, 4H), 2.77 (m, 4H), 1.59 (m, 2H), 1.41 (s, 9H), 0.78 (m, 3H). MS=549 (MH)+.

Provenance & Evidence