1,1-Dimethylethyl 1-[(1-amino-6-isoquinolinyl)methyl]-2-oxo-2-(1-piperidinyl)ethyl-carbamate → (2S)-N-[1-[(1-amino-6-isoquinolinyl)methyl]-2-oxo-2-(1-piperidinyl)ethyl]-4-(4-morpholinyl)-4-oxo-2-[(4-methoxy-2,3,6-trimethylphenylsulfonyl)amino]butanamide hydrochloride

Participants

Reaction Steps

The procedure described for 5c was used. Deprotection of 5a and coupling with 51a yielded after purification the title compound (79%) as a mixture of diastereomers (1:1). 1H-NMR 200 MHz (CD3OD) δ: 1.30-1.51 (6H, m), 2.14 (3H, s), 2.51 and 2.53 (3H, 2× s,), 2.63 (3H, s), 2.31-3.62 (16H, m), 3.84 and 3.86 (3H, 2× s), 3.99-4.15 (1H, m), 5.08-5.21 (1H, m), 6.75 and 6.76 (1H, 2× s), 7.18-7.25 (1H, m), 7.52-7.81 (3H, m), 8.25-8.37 (1H, m).

Provenance & Evidence