반응 #326179

반응 방정식

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

3-aminophenyl acetylene

tartaric acid

→

erlotinib base

Erlotinib Hydrochloride

용매

ethanol

반응 조건

후처리

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

실험 절차

15.0 g of 4-chloro-6,7-bis(2-methoxyethoxy) quinazoline was suspended in 450 ml ethanol and 13.8 g of 3-aminophenyl acetylene was added at 25-30° C. Further 3.0 g tartaric acid was added. The reaction mass was stirred at 25-30° C. for 6 hours. Solid obtained was filtered, washed with water and dried under vacuum. This solid was suspended in water, basified with potassium hydroxide and stirred for 10 minutes. The resulting erlotinib base was isolated by filtration, washed with ethanol and dried under vacuum. The solid obtained was then 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 at 40-45° C. to obtain 18.3 g of erlotinib hydrochloride.

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