Chloroacetyl chloride → 4-Amino-6,7-dimethoxy-2-[4-chloroacetyl-(+/-)-cis-octahydro-1-quinoxalinyl]-quinazoline hydrochloride

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Reaction Steps

A solution of 0.26 g of chloroacetyl chloride in 6 ml of methylene chloride was added dropwise over 15 minutes at 0° C. to a stirred mixture of 0.5 g of the above intermediate 4A and 0.21 g of diisopropylethylamine in 15 ml of methylene chloride. After 4-hour stirring at room temperature and 72-hour resting in a refrigerator, the solid was collected by suction and purified by crystallisation from chloroform to give 0.12 g (33%) of the desired product; m.p. >270° C.

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