Water → HCID 56943579, 화합물

HRID 1631152노트

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HRID 1631152 반응식
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

참가 물질

7

반응물 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, 화합물

생성물 1

HCID 56943579HCID 56943579, 화합물

시약·촉매·용매 2

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

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온도
120 °C

실험 절차

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).

후처리

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

출처 및 근거

ORD 기록
ord-85d9849f38f348b4b6c2a70fca72fcbd
출처 데이터셋
uspto-grants-2014_07
특허 번호
US08791129B2

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