Reaction of theophylline (I) with 1,3-dibromopropane (II) in DMF in the presence of triethylamine afforded the bromo intermediate (III)) in 77% yield. Reaction of (III) with 4-hydroxypiperidine (IV) in DMF in the presence of sodium bicarbonate afforded the unsubstituted hydroxypiperidinyl intermediate (V) in 31% yield which was subsequently alkylated with diphenylmethylbromide (VI) to afford Wy-49,051 in 29% yield.

Reaction of theophylline (I) with 1,3-dibromopropane (II) in DMF in the presence of triethylamine afforded the bromo intermediate (III)) in 77% yield. Reaction of (III) with 4-hydroxypiperidine (IV) in DMF in the presence of sodium bicarbonate afforded the unsubstituted hydroxypiperidinyl intermediate (V) in 31% yield which was subsequently alkylated with diphenylmethylbromide (VI) to afford Wy-49,051 in 29% yield.