Reaktion #1010617

Reaktionsgleichung

product

(S)-1-phenylethyl 2-bromo-2-phenylacetate

triethylamine

4,4-difluoropiperidine hydrochloride

→

title compound

Ausbeute 92.4%

(S)-1-phenylethyl 2-(4,4-difluoropiperidin-1-yl)-2-phenylacetate

Ausbeute 92.4%

Lösungsmittel

tetrahydrofuran

THF

Reaktionsbedingungen

Aufarbeitung

1. 1
   workup.STIRRINGThe mixture was stirred for 1 hour at room temperature
2. 2
   WaschenThe cooled mixture was washed with brine
3. 3
   Einengenconcentrated
4. 4
   Sonstigepurified by column chromatography (EtOAc-hexane)

Vorschrift

To a solution of the product from Example 138A (1.00 g, 3.13 mmol) in tetrahydrofuran (20 mL) at room temperature was added triethylamine (1.75 mL, 12.5 mmol) and tetrabutylammonium iodide (0.46 g, 1.25 mmol). The mixture was stirred for 5 minutes and then 4,4-difluoropiperidine hydrochloride (0.74 g, 4.70 mmol) was added as the free base in THF. The mixture was stirred for 1 hour at room temperature and then heated to 55° C. overnight. The cooled mixture was washed with brine, concentrated, then purified by column chromatography (EtOAc-hexane) to provide the title compound (1.04 g, 92% yield).

Quelle