1-(Bromomethyl)-4-chlorobenzene → 1-(4-chlorobenzyl)-5-((4-fluorophenyl)(methyl)amino)pyridin-2(1H)-one

HRID 1948265

반응식

HRID 1948265 반응식
[F:1][C:2]1[CH:7]=[CH:6][C:5]([N:8]([CH3:17])[C:9]2[CH:10]=[N:11][C:12]([O:15]C)=[CH:13][CH:14]=2)=[CH:4][CH:3]=1.[Cl:18][C:19]1[CH:26]=[CH:25][C:22]([CH2:23]Br)=[CH:21][CH:20]=1>C(#N)C>[Cl:18][C:19]1[CH:26]=[CH:25][C:22]([CH2:23][N:11]2[CH:10]=[C:9]([N:8]([C:5]3[CH:6]=[CH:7][C:2]([F:1])=[CH:3][CH:4]=3)[CH3:17])[CH:14]=[CH:13][C:12]2=[O:15])=[CH:21][CH:20]=1

참가 물질

4

반응물 2

HCID 693291-(Bromomethyl)-4-chlorobenzeneHCID 69344815N-(4-fluorophenyl)-6-methoxy-N-methylpyridin-3-amine

생성물 1

HCID 589669221-(4-chlorobenzyl)-5-((4-fluorophenyl)(methyl)amino)pyridin-2(1H)-one수율 34%

시약·촉매·용매 1

HCID 6342Acetonitrile용매

실험 절차

According to Scheme 22 Step 2: The title compound was prepared from N-(4-fluorophenyl)-6-methoxy-N-methylpyridin-3-amine (1 eq, 86 μmol, 20 mg) and 4-chloro-benzylbromide (1.7 eq, 0.15 mmol, 30 mg) according to the procedure described for Example 6 Step 2. Reaction conditions: 12 hours at 80° C. in acetonitrile. The crude product was purified by silica gel chromatography (AIT Flashsmart prepacked column 10 g SiO2) using CH2Cl2/AcOEt 50/50 as eluent to afford 1-(4-chlorobenzyl)-5-((4-fluorophenyl)(methyl)amino)pyridin-2(1H)-one (29 μmol, 10 mg, 34%) as a yellow oil.

후처리

  1. customReaction conditions
  2. custom12 hours
  3. customat 80° C.
  4. customThe crude product was purified by silica gel chromatography (AIT Flashsmart prepacked column 10 g SiO2)

출처 및 근거

ORD 기록
ord-6816c86835b64895996f2da013cdbfcb
출처 데이터셋
uspto-grants-2013_03
특허 번호
US08399493B2

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