Organic Process Research and Development p. 9 - 15 (2001)
Update date:2022-08-30
Topics:
Bridge, Andrew W.
Jones, Ronald H.
Kabir, Humayun
Kee, Alex A.
Lythgoe, David J.
Nakach, Mustafa
Pemberton, Clive
Wrightman, John A.
This contribution describes process improvements to provide a practical and cost-effective synthesis for the manufacture of RG 12525 which resulted in a 3-fold increase in overall yield. Improved solvent systems for chlorination and azidation reactions are described. Adjustments to the tetrazole-forming step eliminated azide sublimation and minimised this risk on scale-up. A robust solvent system was found to control the polymorphic form during crystallisation, which had hitherto been difficult due to the near-equivalence of melting points (154 and 157 °C) of the two known forms.
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