Triethylamine → (R)-tert-Butyl 3-((2S,4S)-1-(4-(5-cyclopropyl-1H-pyrazol-3-ylamino)-6-morpholino-1,3,5-triazin-2-yl)-4-methoxypyrrolidine-2-carboxamido)piperidine-1-carboxylate
반응식
[CH:1]1([C:4]2[NH:8][N:7]=[C:6]([NH:9][C:10]3[N:15]=[C:14]([N:16]4[CH2:21][CH2:20][O:19][CH2:18][CH2:17]4)[N:13]=[C:12]([N:22]4[CH2:26][C@@H:25]([O:27][CH3:28])[CH2:24][C@H:23]4[C:29](O)=[O:30])[N:11]=3)[CH:5]=2)[CH2:3][CH2:2]1.Cl.C(N=C=NCCCN(C)C)C.[NH2:44][C@@H:45]1[CH2:50][CH2:49][CH2:48][N:47]([C:51]([O:53][C:54]([CH3:57])([CH3:56])[CH3:55])=[O:52])[CH2:46]1.O.N1(O)C2C=CC=CC=2N=N1.CCN(CC)CC>CN(C=O)C>[CH:1]1([C:4]2[NH:8][N:7]=[C:6]([NH:9][C:10]3[N:15]=[C:14]([N:16]4[CH2:21][CH2:20][O:19][CH2:18][CH2:17]4)[N:13]=[C:12]([N:22]4[CH2:26][C@@H:25]([O:27][CH3:28])[CH2:24][C@H:23]4[C:29]([NH:44][C@@H:45]4[CH2:50][CH2:49][CH2:48][N:47]([C:51]([O:53][C:54]([CH3:57])([CH3:56])[CH3:55])=[O:52])[CH2:46]4)=[O:30])[N:11]=3)[CH:5]=2)[CH2:3][CH2:2]1참가 물질
7
반응물 5
HCID 8471Triethylamine
HCID 1501974tert-butyl (3R)-3-aminopiperidine-1-carboxylate
HCID 27239391,3-Propanediamine, N'-(ethylcarbonimidoyl)-N,N-dimethyl-, monohydrochloride
HCID 27960291-Hydroxybenzotriazole hydrate
HCID 59436437(2S,4S)-1-(4-(5-Cyclopropyl-1H-pyrazol-3-ylamino)-6-morpholino-1,3,5-triazin-2-yl)-4-methoxypyrrolidine-2-carboxylic acid생성물 1
시약·촉매·용매 1
실험 절차
To a solution of 112B (900 mg, 1.653 mmol) in DMF (10 ml) was added N1-((ethylimino)methylene)-N3,N3-dimethylpropane-1,3-diamine hydrochloride (951 mg, 4.96 mmol), (R)-tert-butyl 3-aminopiperidine-1-carboxylate (993 mg, 4.96 mmol), 1H-benzo[d][1,2,3]triazol-1-ol hydrate (253 mg, 1.653 mmol), and Et3N (1.382 ml, 9.92 mmol). The reaction mixture was stirred at RT for 14 h. The crude reaction mixture was purified by prep. HPLC to give 112C (800 mg, 79%). LC/MS [M+H]+: 613; Ret time (Method F): 2.99 min.
후처리
- customThe crude reaction mixture
- customwas purified by prep
출처 및 근거
- ORD 기록
- ord-0fa755ab9e344469963c1800caca27b5
- 출처 데이터셋
- uspto-grants-2013_04
- 특허 번호
- US08415340B2
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