تفاعل #992771

معادلة التفاعل

2-Cyclopentyl-N-(2-bromo-6-trifluoromethyl-4-morpholin-4-yl-phenyl)-acetamide

3-pyridylboronic acid

potassium carbonate

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title compound

المردود 18.1%

2-Cyclopentyl-N-(4-morpholin-4-yl-2-pyridin-3-yl-6-trifluoromethylphenyl)-acetamide

المردود 18.1%

المذيبات

acetone

ظروف التفاعل

المعالجة

1. 1
   ترشيحThe reaction mixture was filtered through silica (500 mg)
2. 2
   تركيزconcentrated in vacuo
3. 3
   workup.DISSOLUTIONredissolved in dimethyl sulfoxide (0.5 mL)
4. 4
   أخرىsubjected to preparative LC-MS purification

الإجراء التجريبي

2-Cyclopentyl-N-(2-bromo-6-trifluoromethyl-4-morpholin-4-yl-phenyl)-acetamide (1b, 15 mg), 3-pyridylboronic acid (21 mg), aqueous potassium carbonate (5 M, 90 μL) and palladium(II) acetate (1 mg) were mixed in acetone (2 mL) and heated to 130° C. for 20 minutes in a sealed microwave process vial. The reaction mixture was filtered through silica (500 mg), concentrated in vacuo, redissolved in dimethyl sulfoxide (0.5 mL) and subjected to preparative LC-MS purification to furnish 2.7 mg (18% yield) of the title compound as a colorless oil. LC-MS (m/z) 434 (MH+); tR=1.89, (UV, ELSD) 99%, 99%.

المصدر