Hydrochloric Acid → N-(7-(2-Fluoro-4-iodophenylamino)-8-fluoro-4-methylquinazolin-6-yl)-1-(2-hydroxyethyl)cyclopropane-1-sulfonamide

HRID 1161841ノート

反応式

HRID 1161841 の反応式
[F:1][C:2]1[CH:7]=[C:6]([I:8])[CH:5]=[CH:4][C:3]=1[NH:9][C:10]1[C:19]([F:20])=[C:18]2[C:13]([C:14]([CH3:21])=[N:15][CH:16]=[N:17]2)=[CH:12][C:11]=1[NH:22][S:23]([C:26]1([CH2:29][CH2:30][O:31][Si](C(C)(C)C)(C)C)[CH2:28][CH2:27]1)(=[O:25])=[O:24].Cl>C1COCC1>[F:1][C:2]1[CH:7]=[C:6]([I:8])[CH:5]=[CH:4][C:3]=1[NH:9][C:10]1[C:19]([F:20])=[C:18]2[C:13]([C:14]([CH3:21])=[N:15][CH:16]=[N:17]2)=[CH:12][C:11]=1[NH:22][S:23]([C:26]1([CH2:29][CH2:30][OH:31])[CH2:28][CH2:27]1)(=[O:24])=[O:25]

参加物

4

反応物 2

HCID 313Hydrochloric AcidHCID 59519447N-(7-(2-Fluoro-4-iodophenylamino)-8-fluoro-4-methylquinazolin-6-yl)-1-(2-(tert-butyldimethylsilyloxy)ethyl)cyclopropane-1-sulfonamide

生成物 1

HCID 25161112N-(7-(2-Fluoro-4-iodophenylamino)-8-fluoro-4-methylquinazolin-6-yl)-1-(2-hydroxyethyl)cyclopropane-1-sulfonamide

試薬・触媒・溶媒 1

HCID 8028Tetrahydrofuran溶媒

実験手順

To a solution of N-(7-(2-fluoro-4-iodophenylamino)-8-fluoro-4-methylquinazolin-6-yl)-1-(2-(tert-butyldimethylsilyloxy)ethyl)cyclopropane-1-sulfonamide (36 mg, 0.056 mmol) in THF (2 ml) is added HCl (0.18 ml, 1.2 N in H2O, 0.22 mmol). After stirring for 1 h, the reaction is quenched with saturated aqueous NaHCO3 solution (3 ml) and extracted with EtOAc (2×10 ml). The combined organic solution is dried over Na2SO4 and concentrated. Silica gel chromatography yields the title compound.

後処理

  1. customthe reaction is quenched with saturated aqueous NaHCO3 solution (3 ml)
  2. extractionextracted with EtOAc (2×10 ml)
  3. dry with materialThe combined organic solution is dried over Na2SO4
  4. concentrationconcentrated

出典と根拠

ORDレコード
ord-1708dc68f5454cc097cc854747776c8d
出典データセット
uspto-grants-2010_10
特許番号
US07820664B2

反応ノート

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