Water → HCID 56943579、化合物

HRID 1631152ノート

反応式

HRID 1631152 の反応式
Br[C:2]1[CH:15]=[C:14]([F:16])[C:13]([F:17])=[CH:12][C:3]=1[CH2:4][N:5]1[CH:9]([CH3:10])[CH2:8][CH2:7][CH:6]1[CH3:11].C(=O)([O-])[O-].[K+].[K+].O.[NH2:25][C:26]1[N:35]=[C:34]([C:36]([N:38]2[CH2:46][C:45]3[C:40](=[CH:41][CH:42]=[CH:43][CH:44]=3)[CH2:39]2)=[O:37])[C:33]2[C:28](=[CH:29][CH:30]=[C:31](B3OC(C)(C)C(C)(C)O3)[CH:32]=2)[N:27]=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]>[NH2:25][C:26]1[N:35]=[C:34]([C:36]([N:38]2[CH2:39][C:40]3[C:45](=[CH:44][CH:43]=[CH:42][CH:41]=3)[CH2:46]2)=[O:37])[C:33]2[C:28](=[CH:29][CH:30]=[C:31]([C:2]3[CH:15]=[C:14]([F:16])[C:13]([F:17])=[CH:12][C:3]=3[CH2:4][N:5]3[CH:9]([CH3:10])[CH2:8][CH2:7][CH:6]3[CH3:11])[CH:32]=2)[N:27]=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 66836638HCID 66836638、化合物

生成物 1

HCID 56943579HCID 56943579、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

143 mg of 1-(2-bromo-4,5-difluorobenzyl)-2,5-dimethylpyrrolidine, 100 mg of potassium carbonate, 7 μl of water and 17 mg of [1,1′-bis(diphenylphosphino)ferrocene]palladium(II) dichloride are added to a solution of 150 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 4 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-85d9849f38f348b4b6c2a70fca72fcbd
出典データセット
uspto-grants-2014_07
特許番号
US08791129B2

反応ノート

読み込み中…