Dimethylformamide → 2'-Fluoro-5-(5-methyl-pyridin-2-yl)-6'-trifluoromethyl-biphenyl-3-carboxylic acid ((R)-1-methyl-2-morpholin-4-yl-ethyl)-amide
反応式
[F:1][C:2]1[CH:7]=[CH:6][CH:5]=[C:4]([C:8]([F:11])([F:10])[F:9])[C:3]=1[C:12]1[CH:17]=[C:16]([C:18]2[CH:23]=[CH:22][C:21]([CH3:24])=[CH:20][N:19]=2)[CH:15]=[C:14]([C:25]([OH:27])=O)[CH:13]=1.Cl.[O:29]1[CH2:34][CH2:33][N:32]([CH2:35][C@@H:36]([NH2:38])[CH3:37])[CH2:31][CH2:30]1.F[P-](F)(F)(F)(F)F.C[N+](C)=C(N(C)C)ON1C2N=CC=CC=2N=N1.C(N(CC)C(C)C)(C)C.CN(C)C=O>>[CH3:37][C@@H:36]([NH:38][C:25]([C:14]1[CH:13]=[C:12]([C:3]2[C:4]([C:8]([F:9])([F:10])[F:11])=[CH:5][CH:6]=[CH:7][C:2]=2[F:1])[CH:17]=[C:16]([C:18]2[CH:23]=[CH:22][C:21]([CH3:24])=[CH:20][N:19]=2)[CH:15]=1)=[O:27])[CH2:35][N:32]1[CH2:33][CH2:34][O:29][CH2:30][CH2:31]1参加物
6
反応物 5
HCID 6228Dimethylformamide
HCID 81531Diisopropylethylamine
HCID 9886157Methanaminium, N-((dimethylamino)(3H-1,2,3-triazolo(4,5-b)pyridin-3-yloxy)methylene)-N-methyl-, hexafluorophosphate(1-) (1:1)
HCID 673043082'-Fluoro-5-(5-methylpyridin-2-yl)-6'-(trifluoromethyl)biphenyl-3-carboxylic acid
HCID 67387737(S)-1-Morpholinopropan-2-amine hydrochloride生成物 1
実験手順
A round bottom flask was charged with 2′-fluoro-5-(5-methylpyridin-2-yl)-6′-(trifluoromethyl)biphenyl-3-carboxylic acid (100.00 mg, 0.26644 mmol), (S)-1-morpholinopropan-2-amine hydrochloride (112.10 mg, 0.62047 mmol), N,N,N′,N′-tetramethyl-O-(7-azabenzotriazol-1-yl)uronium hexafluorophosphate (0.49150 g, 1.2926 mmol), N,N-diisopropylethylamine (0.36025 mL, 2.0682 mmol), N,N-dimethylformamide (0.882 mL, 11.4 mmol) and the reaction stirred over night at room temperature. The solvent was removed under reduced pressure and the residue purified by prep HPLC to get the compound as white solid.
後処理
- customThe solvent was removed under reduced pressure
- customthe residue purified by prep HPLC
出典と根拠
- ORDレコード
- ord-3da76e04e2c9422b894023fc7bb91f22
- 出典データセット
- uspto-grants-2015_09
- 特許番号
- US09133122B2
反応ノート
読み込み中…