3-AMINOMETHYL-2-BOC-3,4-DIHYDRO-1H-ISOQUINOLINE synthesis

Yield:690244-91-8 84%

Reaction Conditions:

with potassium carbonate in methanol;water at 20; for 56 h;

Steps:

7 Description 7: 3-Aminomethyl-3, 4-DIHYDRO-LH-ISOQUINOLINE-2-CARBOXYLIC acid TERT- butyl ester

A mixture of the amide from D6 (1.18g, 3. 2MMOL), 1M potassium carbonate (15ML) and methanol (40ML) was stirred at room temperature for 56h. Methanol was evaporated in vacuo and the residue partitioned between water and chloroform. The aqueous phase was reextracted with chloroform and the combined extracts dried and evaporated to afford the title product (0.7g, 84%) as a brown OIL. 1H NMR (CDC13) 8 : 1.19-1. 28 (2H, br s), 1.50 (9H, s), 2.55-2. 60 (1H, m), 2.66-2. 71 (1H, m), 2.75-2. 79 (1H, m), 3.02-3. 08 (1H, m), 4.22-4. 26 (1H, m), 4.20-4. 50 (1H, br s), 4.79-4. 82 (1H, m), 7.10-7. 20 (4H, m).

References:

WO2004/41816,2004,A1 Location in patent:Page 15