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

HRID 1517462ノート

反応式

HRID 1517462 の反応式
[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

参加物

4

反応物 2

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

生成物 1

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

試薬・触媒・溶媒 1

HCID 8028Tetrahydrofuran溶媒

実験手順

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]+.

後処理

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

出典と根拠

ORDレコード
ord-5e6d90416e8a46138dd251a5b653c485
出典データセット
uspto-grants-2012_07
特許番号
US08232278B2

反応ノート

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