Maleic Acid → Sunitinib Malate

HRID 1500395

反応式

HRID 1500395 の反応式
[CH3:1][CH2:2][N:3]([CH2:6][CH2:7][NH:8][C:9]([C:11]1[C:12]([CH3:29])=[C:13](/[CH:17]=[C:18]2/[C:19]3[CH:20]=[C:21]([F:28])[CH:22]=[CH:23][C:24]=3[NH:25][C:26]/2=[O:27])[NH:14][C:15]=1[CH3:16])=[O:10])[CH2:4][CH3:5].[C:30]([OH:37])(=[O:36])/[CH:31]=[CH:32]\[C:33]([OH:35])=[O:34]>CO.ClCCl>[CH3:1][CH2:2][N:3]([CH2:6][CH2:7][NH:8][C:9]([C:11]1[C:12]([CH3:29])=[C:13](/[CH:17]=[C:18]2/[C:19]3[CH:20]=[C:21]([F:28])[CH:22]=[CH:23][C:24]=3[NH:25][C:26]/2=[O:27])[NH:14][C:15]=1[CH3:16])=[O:10])[CH2:4][CH3:5].[CH2:31]([C:30]([OH:37])=[O:36])[C@H:32]([OH:10])[C:33]([OH:35])=[O:34]

参加物

5

反応物 2

HCID 444266Maleic AcidHCID 5329102Sunitinib

生成物 1

HCID 6456015Sunitinib Malate収率 89%

試薬・触媒・溶媒 2

HCID 887Methanol溶媒HCID 6344Dichloromethane溶媒

反応条件

温度
27.5 °C

実験手順

Sunitinib (2.0 g) was suspended in 10% methanol in dichloromethane at 25° C. , followed by addition of maleic acid (0.58 g) .The reaction mass was maintained under stirring at 25-30° C. for 60 minutes. The solids obtained were filtered, suck dried and dried under vacuum for a period of 10 hrs at 60° C. to obtain sunitinib maleate. (2.3 g; yield: 89%)

後処理

  1. temperaturewas maintained
  2. customThe solids obtained
  3. filtrationwere filtered
  4. customsuck dried
  5. customdried under vacuum for a period of 10 hrs at 60° C.

出典と根拠

ORDレコード
ord-8d00f1b7495c4220923c190eecedc582
出典データセット
uspto-grants-2015_12
特許番号
US09206163B2

関連ノート

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