1-[2-(4-Iodophenoxy)ethyl]-4-methylpiperidin-4-ol → 1-(2-{4-[5-(4-Chloro-2-methylphenyl)pyrazin-2-ylethynyl]phenoxy}ethyl)-4-methylpiperidin-4-ol

Participants

Reaction Steps

The product was prepared analogously to Example 48.1c from 200 mg (0.88 mmol) of 2-(4-chloro-2-methylphenyl)-5-ethynylpyrazine and 316 mg (0.88 mmol) of 1-[2-(4-iodophenoxy)ethyl]-4-methylpiperidin-4-ol (IP 15) (stirring the reaction mixture overnight at RT). Yield: 30 mg (7% of theoretical); C27H28ClN3O2 (M=461.983); calc.: molpeak (M+H)+:462/464 (Cl); found: molpeak (M+H)+:462/464 (Cl); HPLC-MS: 5.43 minutes (method G; Zorbax-Bonus).

Provenance & Evidence