合成路线1

Elesclomol can be prepared as follows. The precursor thiobenzoic acid N-methylhydrazide (III) can be obtained by either treatment of carboxymethyl dithiobenzoate (I) with methylhydrazine under alkaline conditions or by reaction of phenylmagnesium bromide (II) with carbon disulfide, followed by treatment with methylhydrazine. Then, dimerization of thiohydrazide (III) with malonic acid in the presence of DCC/HOBt, or with malonyl dichloride or malonic acid diphenyl ester, provides the target malonohydrazide derivative (1, 2). Conversion of elesclomol to different salts (including sodium, potassium, lithium, calcium, magnesium, ethanolamine and choline salts) has also been reported (3). Scheme 1.