Tetrahydrofuran → 2-(6-{4-[4-(4-Fluoro-benzyl)-phthalazin-1-yl]-piperazin-1-yl}-pyridin-3-yl)-propan-2-ol

HRID 42208

반응식

HRID 42208 반응식
C(OC(=O)[C:5]1[CH:10]=[CH:9][C:8]([N:11]2[CH2:16][CH2:15][N:14]([C:17]3[C:26]4[C:21](=[CH:22][CH:23]=[CH:24][CH:25]=4)[C:20]([CH2:27][C:28]4[CH:33]=[CH:32][C:31]([F:34])=[CH:30][CH:29]=4)=[N:19][N:18]=3)[CH2:13][CH2:12]2)=[N:7][CH:6]=1)C.[CH3:36][Mg]I.[CH2:39]1[CH2:43][O:42]CC1>>[F:34][C:31]1[CH:32]=[CH:33][C:28]([CH2:27][C:20]2[C:21]3[C:26](=[CH:25][CH:24]=[CH:23][CH:22]=3)[C:17]([N:14]3[CH2:13][CH2:12][N:11]([C:8]4[N:7]=[CH:6][C:5]([C:43]([OH:42])([CH3:39])[CH3:36])=[CH:10][CH:9]=4)[CH2:16][CH2:15]3)=[N:18][N:19]=2)=[CH:29][CH:30]=1

참가 물질

4

반응물 3

HCID 8028TetrahydrofuranHCID 592406536-{4-[4-(4-Fluoro-benzyl)-phthalazin-1-yl]-piperazin-1-yl}-nicotinic acid ethyl esterHCID 178418373HCID 178418373, 화합물

생성물 1

HCID 592405842-(6-{4-[4-(4-Fluoro-benzyl)-phthalazin-1-yl]-piperazin-1-yl}-pyridin-3-yl)-propan-2-ol수율 10%

실험 절차

6-{4-[4-(4-Fluoro-benzyl)-phthalazin-1-yl]-piperazin-1-yl}-nicotinic acid ethyl ester (85 mg, 0.180 mmol) is dissolved in THF (1 mL). Methyl magnesium iodide (240 μL, 3M in diethyl ether, 0.72 mmol) is added dropwise. Stir reaction for 2 h at room temperature. Concentrate in vacuo. The residue is purified by flash chromatography on silica gel (MeOH/CH2Cl2) to afford the title compound (8 mg, 10%).

후처리

  1. customreaction for 2 h at room temperature
  2. concentrationConcentrate in vacuo
  3. customThe residue is purified by flash chromatography on silica gel (MeOH/CH2Cl2)

출처 및 근거

ORD 기록
ord-ea976603e2204ac9bd075527618ef6cc
출처 데이터셋
uspto-grants-2013_09
특허 번호
US08536168B2

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