Reaktion #1777083

Reaktionsgleichung

4-(2-methoxy-ethylamino)-piperidine-1-carboxylic acid tert-butyl ester

2-bromopropane

potassium carbonate

→

4-[isopropyl-(2-methoxy-ethyl)-amino]-piperidine-1-carboxylic acid tert-butyl ester

Lösungsmittel

DCM

MeCN

Reaktionsbedingungen

Aufarbeitung

1. 1
   TemperaturThe reaction mixture was cooled down
2. 2
   Waschenwashed with brine
3. 3
   Trocknendried (MgSO4)
4. 4
   Sonstigethe solvent removed in vacuo
5. 5
   SonstigeThe residue was purified

Vorschrift

Amine preparation: A mixture of 4-(2-methoxy-ethylamino)-piperidine-1-carboxylic acid tert-butyl ester (see preparation of 121) (300 mg) and 2-bromopropane (1.20 mL) in MeCN (3 mL) with potassium carbonate (192 mg) were heated at 60° C. in a sealed tube for 7 days. The reaction mixture was cooled down, diluted with DCM, washed with brine, dried (MgSO4) and the solvent removed in vacuo. The residue was purified using flash chromatography to yield 4-[isopropyl-(2-methoxy-ethyl)-amino]-piperidine-1-carboxylic acid tert-butyl ester as an oil (131 mg). Treatment of this compound with HCl in DCM/MeOH and basic wash with aqueous sodium bicarbonate yielded the desired amine.

Quelle