Toluene → 2-(4-Bromo-3-fluoro-phenyl)-pyrimidine

HRID 1038115노트

반응식

HRID 1038115 반응식
[Br:1][C:2]1[CH:7]=[CH:6][C:5](B(O)O)=[CH:4][C:3]=1[F:11].Br[C:13]1[N:18]=[CH:17][CH:16]=[CH:15][N:14]=1.C(=O)([O-])[O-].[Na+].[Na+].C1(C)C=CC=CC=1>C(O)C>[Br:1][C:2]1[CH:7]=[CH:6][C:5]([C:13]2[N:18]=[CH:17][CH:16]=[CH:15][N:14]=2)=[CH:4][C:3]=1[F:11]

참가 물질

6

반응물 4

HCID 1140TolueneHCID 10340Sodium CarbonateHCID 783452-BromopyrimidineHCID 27733354-Bromo-3-fluorobenzeneboronic acid

생성물 1

HCID 576858522-(4-Bromo-3-fluoro-phenyl)-pyrimidine

시약·촉매·용매 1

HCID 702Ethanol용매

실험 절차

4-Bromo-3-fluorophenyl boronic acid (28AB) (1.0 g, 4.57 mmol, 1 equiv), 2-bromopyrimidine (1AB) (2.18 g, 13.7 mmol, 3 equiv), and 2M sodium carbonate (12 mL) were added in a pressure vessel (150 mL) and a (1v:1v) mixture of toluene and ethanol (25 mL: 25 mL) was added. The mixture was then bubbled with nitrogen gas for about 10 minutes. Tetrakistriphenylphosphine palladium (0) (266 mg, 0.23 mmol, 0.05 equiv) was added to the mixture. The reaction vessel was tightly capped, placed in an oil bath at 90° C., and stirred overnight.

후처리

  1. additionwas added
  2. customThe mixture was then bubbled with nitrogen gas for about 10 minutes
  3. customThe reaction vessel was tightly capped
  4. customplaced in an oil bath at 90° C.

출처 및 근거

ORD 기록
ord-7c8ac1affafc4d6da345ab1fe5c347f3
출처 데이터셋
uspto-grants-2013_10
특허 번호
US08546404B2

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