Trisubstituted 3,4-dihydro-1H-isoquinolin compound, process for its preparation, and its use

1. Compound of formula 7*acetate

2. Process for the preparation of the compound of formula 7*acetate

which process comprises the reaction of the compound of formula 7

with acetic acid, to obtain the compound of formula 7*acetate.

3. Process according to claim 2 , for the preparation of the compound of formula 7*acetate, wherein the compound of formula 7

is prepared by hydrogenation of the compound of formula 4

in the presence of bis[chloro-1,5-cyclooctadiene-iridium], (S)-1-dicyclohexylphosphino-2-[(S)-α-(dimethylamino)-2-(dicyclohexylphosphino)benzyl]-ferrocene, iodine and a solvent, under hydrogen pressure of 1-200 bar, to obtain the compound of formula 7.

4. Process according to claim 3 , for the preparation of the compound of formula 7*acetate, wherein the compound of formula 4

is prepared by reaction of the compound of formula 4*mesylate

with a base, to obtain the compound of formula 4.

5. Process according to claim 2 , wherein the reaction is carried out with 0.9 to 1.3 equivalents of acetic acid.

6. Process according to claim 3 , wherein the amount of iodine compared to the amount of Ir is between 0.2 and 10 mol equivalents.

7. Process according to claim 3 , wherein the molar ratio between Ir and the chiral ligand is between 0.5:1 and 1:0.5.

8. Process according to claim 3 , wherein the hydrogen pressure is between 1 and 50 bar.

9. Process according to claim 4 , wherein the amount of base is between 0.9 and 1.5 mol equivalents.

10. A process for the preparation of compound of formula I*HCl

comprising:

a) reacting the compound of formula 7*acetate,

with a base to obtain the compound of formula 7:

b) reacting the compound of formula 7 with compound of formula 6:

in the presence of a base, to obtain the compound of formula I:

c) reacting the compound of formula I with hydrochloric acid, to obtain the compound of formula I*HCl.