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

HRID 634484노트

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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

참가 물질

실험 절차

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%).

후처리

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%)

출처 및 근거

ORD 기록: ord-9f27113e43bb4a8d98415ea5bcac342c
출처 데이터셋: uspto-grants-2016_04
DOI: 10.6084/m9.figshare.5104873.v1
특허 번호: US09321776B2

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