N

The second way differs from the first in that the methylation of nitrogen is accomplished before the cyclocondensation reaction. In order to do this, the initial 2-amino-5-chlorobenzo-phenone is first tosylated by p-toluenesulfonylchloride and the obtained tosylate (5.1.3) transformed into the N-sodium salt, which is then alkylated by dimethylsulfate. The resulting 2-N-tosyl-N-methyl-5-chlorobenzophenone (5.1.4) is hydrolyzed in an acidic medium, giving 2-methylamino-5-chlorobenzophenone (5.1.5), which undergoes cyclocondensation by reaction with ethyl ester of glycine hydrochloride, forming the desired diazepam (5.1.2) [1-5].

(CH3O)2SO2

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