Potassium Cyanide → 2-(5-(3-Amino-4-fluoro-1-(3-(pyrimidin-5-yl)phenyl)-1H-isoindol-1-yl)-2-methoxy-3-methylphenyl) acetonitrile

HRID 1662266노트

반응식

HRID 1662266 반응식
Br[CH2:2][C:3]1[CH:4]=[C:5]([C:12]2([C:23]3[CH:28]=[CH:27][CH:26]=[C:25]([C:29]4[CH:30]=[N:31][CH:32]=[N:33][CH:34]=4)[CH:24]=3)[C:20]3[C:15](=[C:16]([F:21])[CH:17]=[CH:18][CH:19]=3)[C:14]([NH2:22])=[N:13]2)[CH:6]=[C:7]([CH3:11])[C:8]=1[O:9][CH3:10].[C-:35]#[N:36].[K+]>CC#N>[NH2:22][C:14]1[C:15]2[C:20](=[CH:19][CH:18]=[CH:17][C:16]=2[F:21])[C:12]([C:5]2[CH:6]=[C:7]([CH3:11])[C:8]([O:9][CH3:10])=[C:3]([CH2:2][C:35]#[N:36])[CH:4]=2)([C:23]2[CH:28]=[CH:27][CH:26]=[C:25]([C:29]3[CH:30]=[N:31][CH:32]=[N:33][CH:34]=3)[CH:24]=2)[N:13]=1

참가 물질

4

반응물 2

HCID 9032Potassium CyanideHCID 585794761-(3-(Bromomethyl)-4-methoxy-5-methylphenyl)-4-fluoro-1-(3-(pyrimidin-5-yl)phenyl)-1H-isoindol-3-amine

생성물 1

HCID 585794892-(5-(3-Amino-4-fluoro-1-(3-(pyrimidin-5-yl)phenyl)-1H-isoindol-1-yl)-2-methoxy-3-methylphenyl) acetonitrile수율 13.8%

시약·촉매·용매 1

HCID 6342Acetonitrile용매

실험 절차

To a solution of 1-(3-(bromomethyl)-4-methoxy-5-methylphenyl)-4-fluoro-1-(3-(pyrimidin-5-yl)phenyl)-1H-isoindol-3-amine (185 mg, 0.36 mmol) in MeCN (5 mL) was added potassium cyanide (69.8 mg, 1.07 mmol) and the reaction mixture was stirred at rt over night. The mixture was filtered and the filtrate was concentrated in vacuo and purified by preparative HPLC to give 23 mg (12%) of the title compound.

후처리

  1. filtrationThe mixture was filtered
  2. concentrationthe filtrate was concentrated in vacuo
  3. custompurified by preparative HPLC

출처 및 근거

ORD 기록
ord-f308fd3e6e104544a3f7728addb9a94f
출처 데이터셋
uspto-grants-2011_10
특허 번호
US08030500B2

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