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2-(Di-tert-butylphosphino)biphenyl → 5-Fluoro-2-[[5-methyl-7-[(1-oxothietan-1-ylidene)amino]quinazolin-4-yl]amino]phenol

HRID 2281104
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인쇄 미리보기

반응식

HRID 2281104 반응식
Br[C:2]1[CH:11]=[C:10]2[C:5]([C:6]([NH:12][C:13]3[CH:18]=[CH:17][C:16]([F:19])=[CH:15][C:14]=3[OH:20])=[N:7][CH:8]=[N:9]2)=[C:4]([CH3:21])[CH:3]=1.[NH:22]=[S:23]1(=[O:27])[CH2:26][CH2:25][CH2:24]1.C(P(C(C)(C)C)C1C=CC=CC=1C1C=CC=CC=1)(C)(C)C.CC(C)([O-])C.[Na+]>O1CCOCC1.C1C=CC(/C=C/C(/C=C/C2C=CC=CC=2)=O)=CC=1.C1C=CC(/C=C/C(/C=C/C2C=CC=CC=2)=O)=CC=1.C1C=CC(/C=C/C(/C=C/C2C=CC=CC=2)=O)=CC=1.[Pd].[Pd]>[F:19][C:16]1[CH:17]=[CH:18][C:13]([NH:12][C:6]2[C:5]3[C:10](=[CH:11][C:2]([N:22]=[S:23]4(=[O:27])[CH2:26][CH2:25][CH2:24]4)=[CH:3][C:4]=3[CH3:21])[N:9]=[CH:8][N:7]=2)=[C:14]([OH:20])[CH:15]=1
참가 물질실험 절차후처리출처 및 근거반응 노트

참가 물질

7

반응물 4

HCID 27342152-(Di-tert-butylphosphino)biphenylHCID 216845701-Imino-1lambda6-thietan-1-oneHCID 23676156Sodium t-butoxideHCID 901224722-[(7-Bromo-5-methyl-quinazolin-4-yl)amino]-5-fluoro-phenol

생성물 1

HCID 1177742805-Fluoro-2-[[5-methyl-7-[(1-oxothietan-1-ylidene)amino]quinazolin-4-yl]amino]phenol

시약·촉매·용매 2

HCID 9811564
Bis(dibenzylideneacetone)palladium
촉매
HCID 312751,4-Dioxane용매

실험 절차

1.5 g (4.3 mmol) 2-[(7-bromo-5-methyl-quinazolin-4-yl)amino]-5-fluoro-phenol, 0.45 g (4.3 mmol) 1-iminothietane 1-oxide (IV.6), 0.26 g (0.86 mmol) 2-(di-t-butylphosphino) biphenyl, 0.3 g (0.33 mmol) Pd2dba3 and 0.61 g (6.4 mmol) sodium tert-butoxide in dioxane are heated to 80° C. for 3 h. After cooling to RT the reaction mixture is filtered and evaporated. The residue is purified by FC.

후처리

  1. filtrationis filtered
  2. customevaporated
  3. customThe residue is purified by FC

출처 및 근거

ORD 기록
ord-1c84f241b3364d3fa67417b099ce8b91
출처 데이터셋
uspto-grants-2015_09
DOI
10.6084/m9.figshare.5104873.v1
특허 번호
US09139577B2

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