Реакция #661823

Уравнение реакции

1-[3-(4-fluoro-phenyl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-ethanone

tri-n-butylphosphine

1,1′-(azodicarbonyl)dipiperidine

(S)-1-indanol

→

1-[(R)-3-(4-fluoro-phenyl)-1-indan-1-yl-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-ethanone

1-[(R)-3-(4-Fluoro-phenyl)-1-indan-1-yl-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-ethanone

Растворители

toluene

Условия реакции

Обработка

1. 1
   ДругоеSolvents were evaporated in vacuo
2. 2
   ДругоеThe crude product was purified by reverse phase HPLC (CH3CN/water gradient with 0.1% trifluoroacetic acid)

Методика

According to Scheme 7: A mixture of 1-[3-(4-fluoro-phenyl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-ethanone (3b) (0.2 g, 0.771 mmol), tri-n-butylphosphine (0.312 g, 1.54 mmol), 1,1′-(azodicarbonyl)dipiperidine (0.389 g, 1.54 mmol) and (S)-1-indanol in dry toluene (2.5 ml) was stirred at 80° C. for 2 h. Solvents were evaporated in vacuo. The crude product was purified by reverse phase HPLC (CH3CN/water gradient with 0.1% trifluoroacetic acid) to give 81 mg of 1-[(R)-3-(4-fluoro-phenyl)-1-indan-1-yl-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-ethanone (12a)

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