Reaktion #708

ord-e759a68ff56d4b3bb4604b0f87a340c5

Reaktionsgleichung

COc1ccc(N2CCN(C)CC2)c2c1CCN(C(=O)Cc1ccc(Br)cc1)C2
COc1ccc(N2CCN(C)CC2)
C1CCNCC1
C1CCNCC1
COc1ccc(N2CCN(C)CC2)c2c1CCN(C(=O)Cc1ccc(N3CCCCC3)cc1)C2
COc1ccc(N2CCN(C)CC2)

Lösungsmittel

Reaktionsbedingungen

Temperatur
100°CELSIUS

Vorschrift

2-(4-bromophenyl)-1-(5-methoxy-8-(4-methylpiperazin-1-yl)-3,4-dihydroisoquinolin-2(1H)-yl)ethanone (125 mg, 0.27 mmol),[Reactants],piperidine (23.22 mg, 0.27 mmol) was taken in a mixture of DME (5 mL):water (1.250 mL) under N2.The reaction mixture was purged under N2 for 10 min.Tris(dibenzylideneacetone)dipalladium (0) (14.98 mg, 0.02 mmol) was added to the above reaction.The resulting reaction was stirred for 3 hrs at reflux tempt.LCMS profile showed formation of required product.Reaction was cooled to rt,solvents was evapourated to dryness.Crude was diluted with DCM and water (min) and organic layer separated and concentrated .Purification was done on RP systme to get product 1-(5-methoxy-8-(4-methylpiperazin-1-yl)-3,4-dihydroisoquinolin-2(1H)-yl)-2-(4-(piperidin-1-yl)phenyl)ethanone as a solid.but the product was not submitted due to very less ammount.

Quelle

750 AstraZeneca ELN dataset