1H-1-Benzazepine-1-carboxylic acid, 5-aMino-2,3,4,5-tetrahydro-7-Methyl-8-(trifluoroMethyl)-, 1,1-diMethylethyl ester, (5S)- synthesis

Yield:872624-62-9 99%

Reaction Conditions:

with hydrogen;5%-palladium/activated carbon in methanol at 20; under 1034.32 Torr; for 12 h;

Steps:

3.13

Step 13; Preparation of (S)-tert-Butyl 5-amino-7-methyl-8-trifluoromethyl-2,3,4,5-tetrahydrobenzo[&]azepine-l-carboxylate; Shake a mixture of (S)-te?t-butyl 5-azido-7-memyl-84rifluoromethyl-2,3,4,5-tetrahydrobenzo[b]azepine-l-carboxylate (1.44 g, 3.89 mmol) and 5% palladium oncharcoal (0.15 g, 50% wet) in methanol (50 mL) under 20 psi of hydrogen in a Parr bottleat room temperature for 12 h. Filter the mixture through Celite and remove the solventsunder reduced pressure to provide the title compound as a colorless oil (1.30 g, >99%),which is used in the next step without further purification.

References:

WO2006/2342,2006,A1 Location in patent:Page/Page column 62