Reaktion #71698

Reaktionsgleichung

(2S)-1-[(6-Chloro-2-methyl-3-pyridinyl)carbonyl]-2-methyl-4-{[4-(trifluoromethyl)phenyl]sulfonyl}piperazine

Azetidine

→

title compound

Ausbeute 61.9%

(2S)-1-{[6-(1-Azetidinyl)-2-methyl-3-pyridinyl]carbonyl}-2-methyl-4-{[4-(trifluoromethyl)phenyl]sulfonyl}piperazine hydrochloride

Ausbeute 61.9%

Lösungsmittel

isopropanol

Reaktionsbedingungen

Aufarbeitung

1. 1
   EinengenThe reaction mixture was concentrated
2. 2
   Sonstigeto give the crude material as a colourless gum (˜200 mg)
3. 3
   SonstigeThis was purified by MDAP

Vorschrift

(2S)-1-[(6-Chloro-2-methyl-3-pyridinyl)carbonyl]-2-methyl-4-{[4-(trifluoromethyl)phenyl]sulfonyl}piperazine (may be prepared as described in Example 24) (66 mg, 0.14 mmol) was transferred into a microwave vial as a solution in isopropanol (1.4 ml). Azetidine (0.163 ml, 2.42 mmol) was added and the clear solution was heated in the microwave to 120° C. for 18 h with stirring. LCMS analysis showed >80% conversion. The reaction mixture was concentrated to give the crude material as a colourless gum (˜200 mg). This was purified by MDAP to give the free base of the title compound as a brown gum (45 mg).

Quelle