Reaktion #415470

Reaktionsgleichung

pyridine

2-(7-chloro-1,8-naphthyridin-2-yl)-3-hydroxy-6-trifluoromethyl-1-isoindolinone

1-chlorocarbonyl-4-methyl-piperazine hydrochloride

triethylamine

→

2-(7-chloro1,8-naphthyridin-2-yl)-3-(4-methyl-piperazinyl)carbonyloxy-6-trifluoromethyl-1-isoindolinone

Ausbeute 73.5%

Lösungsmittel

methylene chloride

Reaktionsbedingungen

Aufarbeitung

1. 1
   Sonstigea crude product (7.8 g.) is obtained
2. 2
   Sonstigewhich is triturated with water (50 cc.)
3. 3
   SonstigeThe solid obtained
4. 4
   Filtrationis filtered off
5. 5
   Waschenwashed with water (30 cc.)
6. 6
   SonstigeAfter recrystallisation from isopropanol (240 cc.)

Vorschrift

Following the procedure of Example 28, but starting from 2-(7-chloro-1,8-naphthyridin-2-yl)-3-hydroxy-6-trifluoromethyl-1-isoindolinone (4.8 g.), 1-chlorocarbonyl-4-methyl-piperazine hydrochloride (15.1 g.), triethylamine (14.2 cc., equivalent to 10.2 g.) and pyridine (66 cc.) in methylene chloride (250 cc.), a crude product (7.8 g.) is obtained, which is triturated with water (50 cc.). The solid obtained is filtered off and washed with water (30 cc.). After recrystallisation from isopropanol (240 cc.), 2-(7-chloro1,8-naphthyridin-2-yl)-3-(4-methyl-piperazinyl)carbonyloxy-6-trifluoromethyl-1-isoindolinone (4.7 g.) melting at 219° C is obtained.

Quelle