Potassium Carbonate → 6-(4-Cyclopropylphenyl)-3-(trifluoromethyl)-[1,2,4]triazolo[4,3-a]pyridine

HRID 1846929

反応式

HRID 1846929 の反応式
Br[C:2]1[CH:3]=[CH:4][C:5]2[N:6]([C:8]([C:11]([F:14])([F:13])[F:12])=[N:9][N:10]=2)[CH:7]=1.[CH:15]1([C:18]2[CH:23]=[CH:22][C:21](B(O)O)=[CH:20][CH:19]=2)[CH2:17][CH2:16]1.C(=O)([O-])[O-].[K+].[K+]>C1(C)C=CC=CC=1>[CH:15]1([C:18]2[CH:23]=[CH:22][C:21]([C:2]3[CH:3]=[CH:4][C:5]4[N:6]([C:8]([C:11]([F:14])([F:13])[F:12])=[N:9][N:10]=4)[CH:7]=3)=[CH:20][CH:19]=2)[CH2:17][CH2:16]1

参加物

5

反応物 3

HCID 11430Potassium CarbonateHCID 28494284-Cyclopropylbenzeneboronic acidHCID 581189066-Bromo-3-(trifluoromethyl)-(1,2,4)triazolo(4,3-a)pyridine

生成物 1

HCID 581189736-(4-Cyclopropylphenyl)-3-(trifluoromethyl)-[1,2,4]triazolo[4,3-a]pyridine

試薬・触媒・溶媒 1

HCID 1140Toluene溶媒

反応条件

温度
90 °C

実験手順

A suspension of 6-bromo-3-(trifluoromethyl)-[1,2,4]triazolo[4,3-a]pyridine (50 mg, 0.19 mmol), 4-cyclopropyl phenylboronic acid (34 mg, 0.21 mmol), dppf(Pd)Cl2 (6.9 mg, 0.094 mmol), potassium carbonate (52 mg, 0.62 mmol) in degassed toluene (1 mL), degassed water (0.5 mL) and degassed ethanol (0.5 mL) was heated at 90° C. for 1 hour. The layers are separated, the organic layer was concentrated and the residue was purified by column chromatography to provide 6-(4-cyclopropylphenyl)-3-(trifluoromethyl)-[1,2,4]triazolo[4,3-a]pyridine as a white powder.

後処理

  1. customdegassed water (0.5 mL)
  2. customdegassed ethanol (0.5 mL)
  3. customThe layers are separated
  4. concentrationthe organic layer was concentrated
  5. customthe residue was purified by column chromatography

出典と根拠

ORDレコード
ord-6e3c1ded381f47079938ae53b36e7bb0
出典データセット
uspto-grants-2015_02
特許番号
US08952034B2

関連ノート

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