(3S)-7-nitro-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid synthesis

Yield:77141-07-2 93%

Reaction Conditions:

with sulfuric acid;nitric acid at -20; for 0.5 h;

Steps:

Concentrated HN03(22mL)was added dropwise to a stirred solutionof 9A (30g, 170 mmol)in concentrated H2 S04 (120 mL) at -20°C. The reaction mixture was stirredat -20°C for0.5h then poured into ice water. The mixture was neutralization withammonium hydroxide,then filtered and washed with water to give 9B as a white solid (35 g, 93 %).

References:

WO2015/81891,2015,A1 Location in patent:Page/Page column 143