Racemic (±)<unk>  6 is a white crystalline powder as the hydrochloride hemihydrate m.p. 245 °C. It is a mixture of two enantiomers and is moderately lipophilic (log P = 1.2) with good solubility 80 mg/mL in water at 25 °C. The compound is very stable in the solid state and its bioavailability from tablet formulation is 85% and absorption is rapid. Synthesis Racemic (±)<unk>  6 was first synthesised by a convergent route, which involved converting the bis-benzyl ether of cis-butene-l,4-diol 1 into its epoxide 2 followed by acid catalyzed ring opening to a racemic-diol which was then converted into the racemic trans bis-tosylate 3. Coupling 3-fluorocatechol 4 with the racemic trans bis-tosylate 3 in the presence base gave on deprotection the benzodioxan diol 5 which was converted to racemic 6 via coupling its bis-mesylate to benzylamine followed by deprotection. The Convergent Synthesis of<unk>  The individual chiral isomers (+) 7 and (-) 8 of<unk>  were originally prepared from the (+) and (-) isomers of diethyl tartrate via the corresponding chiral trans bis-tosylates in a convergent route similar to that shown in the synthesis of racemic<unk> .
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