A Greener
Approach for the Large-Scale Synthesis of
1,4,5-Trisubstituted Pyrazole, AZD8329
- Publication date
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Abstract
The
development of a convenient, safe and scalable process for <b>AZD8329</b> manufacturing is reported here. Synthesis was achieved
in a two-step telescopic process with an excellent overall yield of
75%. In the first step enamine (<b>6</b>) was synthesized with
90% yield through three chemical transformations. In the next step <b>AZD8329</b> was synthesized from the reactions of <b>6</b> and 4-hydrazinobenzoic acid hydrochloride <b>7</b> through
two chemical transformations. The process is very efficient and economical,
and <b>AZD8329</b> was manufactured in multikilogram scale.
A greener approach is demonstrated through usage of a minimum number
of solvents and energy and with process mass intensity (PMI) <60
in the manufacturing process
