Triethylamine → 4-(2-piperidinon-1-yl)piperidin-1-yl 2N-(4-chlorophenylaminocarbonyl)-1,2,3,4-tetrahydroisoquinoline-3-carboxamide

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CN1CCN=C1C1C=CC([NH:13][C:14]([C@H:16]2[CH2:25][C:24]3[C:19](=[CH:20][CH:21]=[CH:22][CH:23]=3)[CH2:18][N:17]2[C:26]([NH:28][C:29]2[CH:34]=[CH:33][C:32]([Cl:35])=[CH:31][CH:30]=2)=[O:27])=[O:15])=CC=1.ClC1C=CC(NC(C2C3C(=CC=CC=3)CC(C(O)=O)N2)=O)=CC=1.[N:59]1([CH:66]2[CH2:71][CH2:70][NH:69][CH2:68][CH2:67]2)[CH2:64][CH2:63][CH2:62][CH2:61][C:60]1=[O:65].C(N(CC)CC)C.F[P-](F)(F)(F)(F)F.N1(O[P+](N(C)C)(N(C)C)N(C)C)C2C=CC=CC=2N=N1>CN(C=O)C>[N:59]1([CH:66]2[CH2:71][CH2:70][N:69]([CH:18]3[C:19]4[C:20](=[CH:21][CH:22]=[CH:23][CH:24]=4)[CH2:25][CH:16]([C:14]([NH2:13])=[O:15])[N:17]3[C:26]([NH:28][C:29]3[CH:30]=[CH:31][C:32]([Cl:35])=[CH:33][CH:34]=3)=[O:27])[CH2:68][CH2:67]2)[CH2:64][CH2:63][CH2:62][CH2:61][C:60]1=[O:65]

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실험 절차

To a solution of (3R) 2N-(4-chlorophenylaminocarbonyl)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid (50 mg, 0.15 mmol), 4-(2-piperidinon-1-yl) piperidine (20 mg, 0.11 mmol) and triethylamine (30 uL, 0.22 mmol) in DMF (3 mL), BOP (70 mg, 0.16 mmol) was added. The mixture was stirred at room temperature for 30 min. It was then purified by HPLC to give the titled compound (31 mg). MS 495.2 and 497.2 (M+H, Cl pattern).

후처리

customIt was then purified by HPLC

출처 및 근거

ORD 기록: ord-d89b9e16e02844b08496a6acbc5581b5
출처 데이터셋: uspto-grants-2009_11
DOI: 10.6084/m9.figshare.5104873.v1
특허 번호: US07612089B2

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