1-Hydroxybenzotriazole → 2-amino-N-(1-(1-oxo-4-phenyl-1H-isochromen-3-yl)ethyl)pyrazolo[1,5-a]pyrimidine-3-carboxamide

反応式

Cl.[NH2:2][CH:3]([C:5]1[O:6][C:7](=[O:21])[C:8]2[C:13]([C:14]=1[C:15]1[CH:20]=[CH:19][CH:18]=[CH:17][CH:16]=1)=[CH:12][CH:11]=[CH:10][CH:9]=2)[CH3:4].[NH2:22][C:23]1[C:31]([C:32](O)=[O:33])=[C:26]2[N:27]=[CH:28][CH:29]=[CH:30][N:25]2[N:24]=1.C1C=CC2N(O)N=NC=2C=1.CN(C(ON1N=NC2C=CC=CC1=2)=[N+](C)C)C.F[P-](F)(F)(F)(F)F.CCN(C(C)C)C(C)C>C(Cl)Cl>[NH2:22][C:23]1[C:31]([C:32]([NH:2][CH:3]([C:5]2[O:6][C:7](=[O:21])[C:8]3[C:13]([C:14]=2[C:15]2[CH:20]=[CH:19][CH:18]=[CH:17][CH:16]=2)=[CH:12][CH:11]=[CH:10][CH:9]=3)[CH3:4])=[O:33])=[C:26]2[N:27]=[CH:28][CH:29]=[CH:30][N:25]2[N:24]=1

参加物

実験手順

3-(1-aminoethyl)-4-phenyl-1H-isochromen-1-one hydrochloride (intermediate E2, 50 mg, 0.166 mmol), 2-aminopyrazolo[1,5-a]pyrimidine-3-carboxylic acid (32.5 mg, 0.182 mmol), HOBt (30.4 mg, 0.199 mmol), HBTU (17.25 mg, 0.033 mmol) and DIPEA (61.0 μl, 0.349 mmol) were reacted in DCM (1 ml) at RT for 18 hrs. The crude was purified via reverse phase chromatography with a Biotage C18 30 g SNAP column (Phase A, water 95%, ACN 5%, formic acid 0.1%); Phase B ACN 95%, water 5%, formic acid 0.1%) to give the title compound (20 mg, 28%).

後処理

customThe crude was purified via reverse phase chromatography with a Biotage C18 30 g SNAP column (Phase A, water 95%, ACN 5%, formic acid 0.1%)

出典と根拠

ORDレコード: ord-9f27113e43bb4a8d98415ea5bcac342c
出典データセット: uspto-grants-2016_04
DOI: 10.6084/m9.figshare.5104873.v1
特許番号: US09321776B2

反応ノート

読み込み中…

反応式

参加物

反応物 5

生成物 1

試薬・触媒・溶媒 1

実験手順

後処理

出典と根拠

反応ノート