Process for large-scale production of bms 180048 and analogs

Details Process for large-scale production of bms 180048 and analogs Process for large-scale production of bms 180048 and analogs

C - Chemistry, Metallurgy

07

D

C07D 403/14 (2006.01) C07D 403/12 (2006.01) C07F 7/10 (2006.01)

Patent

CA 2161046

An improved, novel convergent process suitable for large scale preparation of the antimigraine agent 4-(5-methoxy-4-pyrimidinyl)-1-[3- [5-[[(methylamino)sulfonyl]methyl]-1H-indol-3-yl]propyl]piperazine (BMS 180048) and close analogs. The improved process provides efficiencies in handling, purification, and product yield and involves a novel heteroannulation reaction that provides the indole ring moiety and propylpiperazinyl-pyrimidine backbone in a single step.

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