Ammonia → 2H-1,4-Benzodiazepin-2-one, 1,3-dihydro-1-(1-methyl-4-piperidinyl)-5-phenyl-

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Reaction Steps

A solution of 379 mg of the above product 2 in 4 ml of trifluoroacetic acid is refluxed under heating for 16 hours. The reaction mixture is mixed with ice water, basified with ammonia and extracted with methylene chloride. The organic layer is washed with water, dried over anhydrous magnesium sulfate and concentrated. The residue is crystallized from ether-petroleum ether to give 278 mg of 1-(1-methyl-4-piperidinyl)-1,3-dihydro-5-phenyl-2H-1,4-benzodiazepin-2-one 3 as crystals melting at 158°-159° C. The yield is 87%.

Provenance & Evidence