Triethylamine → 4-(3-Morpholinon-4-yl)piperidin-1-yl-2-(2-fluorophenyl)-2-(4-chlorophenylaminocarbonylamino)-acetamide

HRID 2245005ノート

反応式

HRID 2245005 の反応式
[F:1][C:2]1[CH:7]=[CH:6][CH:5]=[CH:4][C:3]=1[CH:8]([NH:12][C:13]([NH:15][C:16]1[CH:21]=[CH:20][C:19]([Cl:22])=[CH:18][CH:17]=1)=[O:14])[C:9]([OH:11])=O.Cl.[N:24]1([CH:31]2[CH2:36][CH2:35][NH:34][CH2:33][CH2:32]2)[CH2:29][CH2:28][O:27][CH2:26][C:25]1=[O:30].C([N:39](CC)CC)C.Cl.N1CCCCC1.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.O>[N:24]1([CH:31]2[CH2:36][CH2:35][N:34]([C:8]([C:3]3[CH:4]=[CH:5][CH:6]=[CH:7][C:2]=3[F:1])([NH:12][C:13]([NH:15][C:16]3[CH:21]=[CH:20][C:19]([Cl:22])=[CH:18][CH:17]=3)=[O:14])[C:9]([NH2:39])=[O:11])[CH2:33][CH2:32]2)[CH2:29][CH2:28][O:27][CH2:26][C:25]1=[O:30]

参加物

8

反応物 5

HCID 8471TriethylamineHCID 151348Benzotriazol-1-yloxy-tris(dimethylamino)phosphonium hexafluorophosphateHCID 2723721Piperidine, hydrochloride (1:1)HCID 532556654-(Piperidin-4-yl)morpholin-3-one hydrochlorideHCID 686957412-(2-Fluorophenyl)-2-(4-chlorophenylaminocarbonylamino)-acetic acid

生成物 1

HCID 686907034-(3-Morpholinon-4-yl)piperidin-1-yl-2-(2-fluorophenyl)-2-(4-chlorophenylaminocarbonylamino)-acetamide収率 26.5%

試薬・触媒・溶媒 2

HCID 962Water溶媒HCID 6228Dimethylformamide溶媒

実験手順

To a solution of 2-(2-fluorophenyl)-2-(4-chlorophenylaminocarbonylamino)-acetic acid (50 mg, 0.15 mmol), 4-(3-morpholinon-4-yl)piperidine hydrochloride (45 mg, 0.20 mmol) and triethylamine (0.086 mL, 0.62 mmol) in DMF (1.0 mL, containing 0.10 mL of H2O to solubilize the piperidine hydrochloride), BOP (100 mg, 0.23 mmol) was added. After being stirred at room temperature for 30 min, the mixture was purified by HPLC to give the titled compound (20 mg). MS 489.4 and 491.4 (M+H, Cl pattern).

後処理

  1. additionwas added
  2. customthe mixture was purified by HPLC

出典と根拠

ORDレコード
ord-b25e3a9f6369479daab1c94275a37dac
出典データセット
uspto-grants-2010_03
特許番号
US07678913B2

反応ノート

読み込み中…