반응 #326178

반응 방정식

4-chloro-6,7-bis(2-methoxyethoxy) quinazoline

3-aminophenyl acetylene

benzoic acid

→

erlotinib base

Erlotinib Hydrochloride

용매

methanol

반응 조건

후처리

1. 1
   기타Solid obtained
2. 2
   여과was filtered
3. 3
   세척washed with methanol
4. 4
   기타dried under vacuum
5. 5
   workup.STIRRINGstirred for 10 minutes

실험 절차

10.0 g of 4-chloro-6,7-bis(2-methoxyethoxy) quinazoline was suspended in 300 ml methanol and 9.2 g of 3-aminophenyl acetylene was charged at 25-30° C. Further 2.0 ml of benzoic acid was added. The reaction mass was stirred at 25-30° C. for 4 hours. Solid obtained was filtered, washed with methanol and dried under vacuum. This solid was suspended in water and then basified with sodium hydroxide and stirred for 10 minutes. The resulting erlotinib base was isolated, washed with water and dried under vacuum. The base was suspended in water and acidified to pH 1.0-2.0 using hydrochloric acid. The reaction mixture was stirred for 2 hours, filtered, washed with water and dried to obtain 11.2 g of erlotinib hydrochloride.

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