7-METHOXY-1,2,3,4-TETRAHYDRO-ISOQUINOLINE HYDROCHLORIDE synthesis

Yield:-

Reaction Conditions:

with hydrogenchloride in diethyl ether;ethyl acetate

Steps:

ZV
To a solution OF 7-METHOXY-3, 4-DIHYDRO-2H-ISOQUINOLIN-1-ONE (200mg) in THF (8mL) is added LiAIH4 (76mg) and stirred for 3hr under reflux, and diluted with THF. The reaction mixture is added sodium sulfate decahydrate and filtration through celite pad. The filtrate is concentrated in vacuo. The residue is dissolved in Et20, then HCI in EtOAc is added the Et20. White precipitate is collected. by filtration to provide the title compound; 1 H NMR (CDCI3, 6 (ppm) ); 2.92 (dd, 2H), 3.30-3. 35 (m, 2H), 3.72 (s, 3H), 4.18-4. 23 (m, 2H), 6.81- 6.86 (m, 2H), 7.12 (d, 1H), 9.45 (brs, 2H).

References:

NOVARTIS AG;NOVARTIS PHARMA GMBH WO2004/69256, 2004, A1 Location in patent:Page/Page column 50