(2-(2-Amino-3-morpholinoquinolin-6-yl)-3-methylphenyl)(pyrazin-2-yl)methanol → 6-(2-Methyl-6-(pyrazin-2-ylmethyl)phenyl)-3-morpholinoquinolin-2-amine

HRID 1029012ノート

反応式

HRID 1029012 の反応式
[NH2:1][C:2]1[C:11]([N:12]2[CH2:17][CH2:16][O:15][CH2:14][CH2:13]2)=[CH:10][C:9]2[C:4](=[CH:5][CH:6]=[C:7]([C:18]3[C:23]([CH3:24])=[CH:22][CH:21]=[CH:20][C:19]=3[CH:25]([C:27]3[CH:32]=[N:31][CH:30]=[CH:29][N:28]=3)O)[CH:8]=2)[N:3]=1>CC(O)C.Cl>[CH3:24][C:23]1[CH:22]=[CH:21][CH:20]=[C:19]([CH2:25][C:27]2[CH:32]=[N:31][CH:30]=[CH:29][N:28]=2)[C:18]=1[C:7]1[CH:8]=[C:9]2[C:4](=[CH:5][CH:6]=1)[N:3]=[C:2]([NH2:1])[C:11]([N:12]1[CH2:17][CH2:16][O:15][CH2:14][CH2:13]1)=[CH:10]2

参加物

4

反応物 1

HCID 53329361(2-(2-Amino-3-morpholinoquinolin-6-yl)-3-methylphenyl)(pyrazin-2-yl)methanol

生成物 1

HCID 533295356-(2-Methyl-6-(pyrazin-2-ylmethyl)phenyl)-3-morpholinoquinolin-2-amine

試薬・触媒・溶媒 2

HCID 313Hydrochloric Acid溶媒HCID 3776Isopropanol溶媒

実験手順

A solution of (2-(2-amino-3-morpholinoquinolin-6-yl)-3-methylphenyl)(pyrazin-2-yl)methanol (0.040 g, 0.094 mmol, prepared as Example 36 above) in i-PrOH and 5N HCl (15 mL) was refluxed for 15 h, or until starting material was consumed. The mixture was brought to RT, carefully washed with 5N NaOH and extracted with DCM. The combined organics were dried over Na2SO4, filtered, concentrated and purified by HPLC to afford a light brown solid as 6-(2-methyl-6-(pyrazin-2-ylmethyl)phenyl)-3-morpholinoquinolin-2-amine. MS (ESI, pos. ion) m/z: 412 (M+1).

後処理

  1. customwas consumed
  2. customwas brought to RT
  3. washcarefully washed with 5N NaOH
  4. extractionextracted with DCM
  5. dry with materialThe combined organics were dried over Na2SO4
  6. filtrationfiltered
  7. concentrationconcentrated
  8. custompurified by HPLC

出典と根拠

ORDレコード
ord-dadd8309185f473997c5711979b742ed
出典データセット
uspto-grants-2014_05
特許番号
US08735384B2

反応ノート

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