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Multi-Kilo Delivery of AMG 925 Featuring a Buchwald-Hartwig Amination and Processing with Insoluble Synthetic Intermediates

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Amgen describes the development of a synthetic route to manufacture the drug candidate AMG 925 on kilogram scale. The synthetic route features a Buchwald-Hartwig amination using BrettPhos as ligand and conducted to afford 12 kg of product in a single batch (scheme).

Yet, the target levels of heavy metal in the drug substance AMG 925 were < 100 ppm, much lower than that found in the crude Buchwald-Hartwig product (700 - 800 ppm).

After the screening of potential scavengers, SiliaMetS Thiourea was selected as the scavenger of choice since it was the most effective. At 100 wt % relative to crude product, in 80 % (v/v) toluene/MeOH and a total of 15 volumes of solvent, it afforded product in 90 % with less than 2 ppm of residual Pd.

Caille, S. et al. Org. Process Res. Dev., 2015, 19, 476 - 485

 

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  1. SiliaMetS Thiourea (THU) (R69530B)

    SiliaMetS Thiourea (THU) (R69530B)

    SiliaMetS Thiourea (Si-THU) is a versatile metal scavenger for all forms of palladium and is widely used in the pharmaceutical industry. It works particularly well in organic solvents. It can also be used to scavenge Ag, Pt, Ru, Rh and Hg. Once complexed with a transition metal, it has been reported as being an effective catalyst.

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