Triethylamine → (1r,2r)-2-Phenyl-cyclopropanecarboxylic acid [2-(3-dimethylaminomethyl-phenyl)-6-oxo-5,6-dihydro-1h-[1,2]diazepino[4,5,6-cd]indol-8-yl]-amide

HRID 720118

반응식

HRID 720118 반응식
[CH3:1][N:2]([CH2:4][C:5]1[CH:6]=[C:7]([C:11]2[NH:12][C:13]3[CH:14]=[C:15]([NH:25][C:26](=[O:38])[C:27]4[CH:32]=[CH:31][CH:30]=[C:29]([C:33](F)(F)F)[C:28]=4F)[CH:16]=[C:17]4[C:23](=[O:24])[NH:22][N:21]=[CH:20][C:19]=2[C:18]=34)[CH:8]=[CH:9][CH:10]=1)[CH3:3].[C:39]1([C@@H]2C[C@H]2C(O)=O)C=CC=C[CH:40]=1.C(N(CC)CC)C.F[P-](F)(F)(F)(F)F.N1(OC(N(C)C)=[N+](C)C)C2N=CC=CC=2N=N1>C(O)(C)C.C(Cl)Cl.CN(C)C=O>[CH3:1][N:2]([CH2:4][C:5]1[CH:6]=[C:7]([C:11]2[NH:12][C:13]3[CH:14]=[C:15]([NH:25][C:26]([C@@H:27]4[CH2:32][C@H:28]4[C:29]4[CH:30]=[CH:31][CH:40]=[CH:39][CH:33]=4)=[O:38])[CH:16]=[C:17]4[C:23](=[O:24])[NH:22][N:21]=[CH:20][C:19]=2[C:18]=34)[CH:8]=[CH:9][CH:10]=1)[CH3:3]

참가 물질

8

실험 절차

Preparation of example 83a from Intermediate 73(d) of Example 73 (0.11 g, 0.33 mmol), (1R,2R)-2-phenyl-cyclopropanecarboxylic acid (0.08 g, 0.5 mmol), triethylamine (0.183 mL, 1.32 mmol), O-(7-azabenzotriazol-1-yl)-N,N,N′,N′-tetramethyluronium hexafluorophosphate (0.188 g, 0.5 mmol) and N,N-dimethylformamide (0.2 M, 1.7 mL) was carried out analogously to Example 11. Silica gel chromatography (90:10 to 80:20 CH2Cl2/2M ammonia in isopropyl alcohol) afforded the title compound (0.12 g) as powder in 76% yield.

출처 및 근거

ORD 기록
ord-ce3e7ad7bb5d4bf8b80f530caaaa50d1
출처 데이터셋
uspto-grants-2006_11
특허 번호
US07132533B2

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