Coupling of N-Boc-(4-cyanophenyl)alanine (I) with N-methyl-N-cyclohexylamine (II) by means of EDC and HOBt gave amide (III). The Boc group of (III) was then removed using a methanolic solution of acetyl chloride to afford amine (IV). Chlorosulfonation of benzocycloheptene (V) afforded a mixture of isomeric sulfonyl chlorides (VI) and (VII). Condensation of this mixture with amine (IV) produced the corresponding sulfonamides, which were separated by column chromatography. The major isomer (VIII) was treated with SH2 and Et3N in pyridine to produce the thioamide (IX). Then, S-methylation of (IX) with MeI, followed by displacement of the methylthio group for hydrazine furnished the target benzamidrazone.