Reaktion #607679

Reaktionsgleichung

tert-butyl 5-(chloromethyl)pyridin-2-ylcarbamate

(S)-3-fluoropyrrolidine

potassium carbonate

sodium iodide

→

119

Ausbeute 61.0%

(S)-tert-butyl 5-((3-fluoropyrrolidin-1-yl)methyl)pyridin-2-ylcarbamate

Ausbeute 61.0%

Lösungsmittel

DMF

Reaktionsbedingungen

Aufarbeitung

1. 1
   FiltrationThe reaction mixture was filtered
2. 2
   Einengenthe filtrate was concentrated in vacuo
3. 3
   workup.ADDITIONH2O (250 mL) was added
4. 4
   Filtrationthe resulting solid was collected by filtration
5. 5
   Waschenrinsed with H2O
6. 6
   Sonstigedried

Vorschrift

A mixture of tert-butyl 5-(chloromethyl)pyridin-2-ylcarbamate 117(9.5 g, 39.1 mmol), (S)-3-fluoropyrrolidine 118 (4.19 g, 47.0 mmol), potassium carbonate (16.2 g, 117 mmol) and sodium iodide (0.586 g, 3.91 mmol) in DMF (150 mL) was stirred at 60° C. for 2 h. The reaction mixture was filtered, and the filtrate was concentrated in vacuo. H2O (250 mL) was added and the resulting solid was collected by filtration, rinsed with H2O and dried to give 119 (7.00 g, 61% yield).

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