Triethylamine → N-cyclopropyl-2-[4-[3-[3-(2,2,2-trifluoroethylcarbamoylamino)phenyl]imidazo[1,2-b]pyridazin-7-yl]pyrazol-1-yl]propanamide

HRID 407028

反応式

HRID 407028 の反応式
[CH:1]1([NH2:4])[CH2:3][CH2:2]1.[F:5][C:6]([F:38])([F:37])[CH2:7][NH:8][C:9]([NH:11][C:12]1[CH:13]=[C:14]([C:18]2[N:22]3[N:23]=[CH:24][C:25]([C:27]4[CH:28]=[N:29][N:30]([CH:32]([CH3:36])[C:33](O)=[O:34])[CH:31]=4)=[CH:26][C:21]3=[N:20][CH:19]=2)[CH:15]=[CH:16][CH:17]=1)=[O:10].F[P-](F)(F)(F)(F)F.N1(O[P+](N(C)C)(N(C)C)N(C)C)C2C=CC=CC=2N=N1.C(N(CC)CC)C>CN(C=O)C>[CH:1]1([NH:4][C:33](=[O:34])[CH:32]([N:30]2[CH:31]=[C:27]([C:25]3[CH:24]=[N:23][N:22]4[C:18]([C:14]5[CH:15]=[CH:16][CH:17]=[C:12]([NH:11][C:9]([NH:8][CH2:7][C:6]([F:38])([F:37])[F:5])=[O:10])[CH:13]=5)=[CH:19][N:20]=[C:21]4[CH:26]=3)[CH:28]=[N:29]2)[CH3:36])[CH2:3][CH2:2]1

参加物

6

反応物 4

HCID 8471TriethylamineHCID 69828CyclopropylamineHCID 151348Benzotriazol-1-yloxy-tris(dimethylamino)phosphonium hexafluorophosphateHCID 679802202-(4-{3-[3-({[(2,2,2-trifluoroethyl)amino]carbonyl}amino)phenyl]imidazo[1,2-b]pyridazin-7-yl}-1H-pyrazol-1-yl)propanoic acid

生成物 1

HCID 57384630N-cyclopropyl-2-[4-[3-[3-(2,2,2-trifluoroethylcarbamoylamino)phenyl]imidazo[1,2-b]pyridazin-7-yl]pyrazol-1-yl]propanamide

試薬・触媒・溶媒 1

HCID 6228Dimethylformamide溶媒

実験手順

Cyclopropylamine (17 μL, 0.24 mmol) was added to a mixture of 2-(4-{3-[3-({[(2,2,2-trifluoroethyl)amino]carbonyl}amino)phenyl]imidazo[1,2-b]pyridazin-7-yl}-1H-pyrazol-1-yl)propanoic acid (0.16 mmol) and benzotriazol-1-yloxytris(dimethylamino)phosphonium hexafluorophosphate (110 mg, 0.24 mmol) in DMF (2.0 mL), followed by triethylamine (45 μL, 0.32 mmol). The reaction mixture was stirred at r.t. for 30 min. The mixture was purified by RP-HPLC (pH=10) to afford the desired product. LCMS (M+H)+: m/z=513.2.

後処理

  1. customThe mixture was purified by RP-HPLC (pH=10)

出典と根拠

ORDレコード
ord-604fed29900f4f8ab83f2e9b565db997
出典データセット
uspto-grants-2014_06
特許番号
US08754114B2

関連ノート

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