Water → HCID 56943216、化合物

HRID 1631146ノート

反応式

HRID 1631146 の反応式
Br[C:2]1[CH:13]=[C:12]([F:14])[C:11]([F:15])=[CH:10][C:3]=1[CH2:4][NH:5][C:6]([CH3:9])([CH3:8])[CH3:7].C(=O)([O-])[O-].[K+].[K+].O.[NH2:23][C:24]1[N:33]=[C:32]([C:34]([N:36]2[CH2:44][C:43]3[C:38](=[CH:39][CH:40]=[CH:41][CH:42]=3)[CH2:37]2)=[O:35])[C:31]2[C:26](=[CH:27][CH:28]=[C:29](B3OC(C)(C)C(C)(C)O3)[CH:30]=2)[N:25]=1>C(O)C.C1C=CC(P(C2C=CC=CC=2)[C-]2C=CC=C2)=CC=1.C1C=CC(P(C2C=CC=CC=2)[C-]2C=CC=C2)=CC=1.Cl[Pd]Cl.[Fe+2]>[NH2:23][C:24]1[N:33]=[C:32]([C:34]([N:36]2[CH2:37][C:38]3[C:43](=[CH:42][CH:41]=[CH:40][CH:39]=3)[CH2:44]2)=[O:35])[C:31]2[C:26](=[CH:27][CH:28]=[C:29]([C:2]3[CH:13]=[C:12]([F:14])[C:11]([F:15])=[CH:10][C:3]=3[CH2:4][NH:5][C:6]([CH3:9])([CH3:8])[CH3:7])[CH:30]=2)[N:25]=1

参加物

7

反応物 4

HCID 962WaterHCID 11430Potassium CarbonateHCID 58457219[2-Amino-6-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)quinazolin-4-yl]-(1,3-dihydroisoindol-2-yl)methanoneHCID 66836579HCID 66836579、化合物

生成物 1

HCID 56943216HCID 56943216、化合物

試薬・触媒・溶媒 2

HCID 178418228Bis(cyclopenta-1,4-dien-1-yl(diphenyl)phosphane);dichloropalladium;iron(2+)触媒HCID 702Ethanol溶媒

反応条件

温度
120 °C

実験手順

184 mg of (2-bromo-4,5-difluorobenzyl)-tert-butylamine, 166 mg of potassium carbonate, 11 μl of water and 25 mg of [1,1′-bis(diphenylphosphino)ferrocene]-palladium(II) dichloride are added to a solution of 250 mg of [2-amino-6-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)quinazolin-4-yl]-(1,3-dihydroisoindol-2-yl)methanone in 10 ml of ethanol under argon. The mixture is heated at 120° C. for 30 min; the hot mixture is filtered through kieselguhr, and the filtrate is evaporated. and purified by chromatography (reversed phase HPLC).

後処理

  1. filtrationthe hot mixture is filtered through kieselguhr
  2. customthe filtrate is evaporated
  3. customand purified by chromatography (reversed phase HPLC)

出典と根拠

ORDレコード
ord-063a21399b7c426a978823c6029bb6f8
出典データセット
uspto-grants-2014_07
特許番号
US08791129B2

反応ノート

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