Piperidine → 1-[5-Methoxy-8-(4-methyl-piperazin-1-yl)-3,4-dihydro-1H-isoquinolin-2-yl]-2-(4-piperidin-1-yl-phenyl)-ethanone

HRID 612

반응식

HRID 612 반응식
C1CCNCC1.COc1ccc(N2CCN(C)CC2)c2c1CCN(C(=O)Cc1ccc(Br)cc1)C2>CC(C)(C)[O-].CC1(C)c2cccc(P(c3ccccc3)c3ccccc3)c2Oc2c(P(c3ccccc3)c3ccccc3)cccc21.COCCOC.O=C(/C=C/c1ccccc1)/C=C/c1ccccc1.O=C(/C=C/c1ccccc1)/C=C/c1ccccc1.O=C(/C=C/c1ccccc1)/C=C/c1ccccc1.[Na+].[Pd].[Pd]>COc1ccc(N2CCN(C)CC2)c2c1CCN(C(=O)Cc1ccc(N3CCCCC3)cc1)C2

참가 물질

7

반응 조건

온도
100 °C

실험 절차

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.

출처 및 근거

ORD 기록
ord-e759a68ff56d4b3bb4604b0f87a340c5
출처 데이터셋
750 AstraZeneca ELN dataset
원본 링크
출처 보기

연결된 노트

불러오는 중…