Sodium Methoxide → 6-(4-Fluorophenyl)-4-methoxypyrido[3,2-d]pyrimidin-2-amine

HRID 1517462노트

반응식

HRID 1517462 반응식
[CH3:1][O-:2].[Na+].Cl[C:5]1[C:6]2[N:18]=[C:17]([C:19]3[CH:24]=[CH:23][C:22]([F:25])=[CH:21][CH:20]=3)[CH:16]=[CH:15][C:7]=2[N:8]=[C:9]([NH:11]C(=O)C)[N:10]=1>C1COCC1>[F:25][C:22]1[CH:21]=[CH:20][C:19]([C:17]2[CH:16]=[CH:15][C:7]3[N:8]=[C:9]([NH2:11])[N:10]=[C:5]([O:2][CH3:1])[C:6]=3[N:18]=2)=[CH:24][CH:23]=1

참가 물질

4

반응물 2

HCID 10942334Sodium MethoxideHCID 57698346N-(4-Chloro-6-(4-fluorophenyl)pyrido[3,2-d]pyrimidin-2-yl)acetamide

생성물 1

HCID 576983386-(4-Fluorophenyl)-4-methoxypyrido[3,2-d]pyrimidin-2-amine수율 82.2%

시약·촉매·용매 1

HCID 8028Tetrahydrofuran용매

실험 절차

Sodium methoxide (0.32 mL, 0.158 mmol; 0.5 N in MeOH) was added to a solution of N-[4-chloro-6-(4-fluoro-phenyl)-pyrido[3,2-d]pyrimidin-2-yl]-acetamide (20 mg, 0.063 mmol) in THF (1.5 mL). After stirring at room temperature for 20 minutes, solvents were concentrated in vacuo and the residue was purified by RP HPLC using a C18 column with a gradient of H2O and 0.1% TFA-acetonitrile, to provide the pure title compound as a white solid (14 mg, yield 50%) which was characterised as follows: MS (m/z) 271.0 [M+H]+.

후처리

  1. concentrationsolvents were concentrated in vacuo
  2. customthe residue was purified by RP HPLC

출처 및 근거

ORD 기록
ord-5e6d90416e8a46138dd251a5b653c485
출처 데이터셋
uspto-grants-2012_07
특허 번호
US08232278B2

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