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
反応式
[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]1参加物
7
反応物 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 acid生成物 1
試薬・触媒・溶媒 1
実験手順
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.
後処理
- customThe crude reaction mixture
- customwas purified by prep
出典と根拠
- ORDレコード
- ord-0fa755ab9e344469963c1800caca27b5
- 出典データセット
- uspto-grants-2013_04
- 特許番号
- US08415340B2
反応ノート
読み込み中…