Реакция #418008

Уравнение реакции

DIPEA

N-ethyl-2-(4-ethynyl-phenyl)-propionamide

2-chloro-5-iodo-pyrimidine

→

2-[4-(2-Chloro-pyrimidin-5-ylethynyl)-phenyl]-N-ethyl-propionamide

Растворители

THF

Условия реакции

Обработка

1. 1
   ФильтрацияAfter that time, the mixture is filtered
2. 2
   Другоеthe solvent is evaporated from the filtrate
3. 3
   ДругоеThe residue is purified by column chromatography (silicia gel; DCM:MeOH gradient 1:0/1:1)

Методика

To 1.10 g (5.46 mmol) N-ethyl-2-(4-ethynyl-phenyl)-propionamide (XVII.1) in 10 mL THF are added 1.31 g (5.46 mmol) 2-chloro-5-iodo-pyrimidine under argon, followed by 0.42 g (0.60 mmol) Pd(PPh3)2Cl2 as catalyst, 57 mg (0.30 mmol) copper(I)iodide and 2.1 mL (12 mmol) DIPEA as base. The mixture is stirred at rt for 4 h. After that time, the mixture is filtered and the solvent is evaporated from the filtrate. The residue is purified by column chromatography (silicia gel; DCM:MeOH gradient 1:0/1:1).

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