Key result
A practical and efficient eight-step process was developed for the preparation of the key intermediate (G) of Apixaban starting from inexpensive 4-chloronitrobenzene and piperidine.
A novel, practical, and efficient eight-step synthesis process for the key intermediate of apixaban was developed, potentially lowering production costs.
New apixaban intermediate synthesis may reduce costs; extends scalable routes for NOAC production.
Apixaban is a highly potent, selective, and efficacious inhibitor of blood coagulation factor Xa. A practical and efficient process has been developed for the preparation of the key intermediate ( G ) of Apixaban. Starting from inexpensive 4-chloronitrobenzene and piperidine, an eight-step procedure for G has been developed. In this case, sodium chlorite is used twice to oxidize the piperidine cycle to the corresponding lactam under a CO 2 atmosphere, resulting in the construction of two lactams. Furthermore, most of these reactions are highly efficient and practical as they occur under mild conditions. Most of the intermediates can be obtained through simple slurry or recrystallization, and column chromatography purification is not necessary.
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Dong et al. (2023) studied this question. Chemical synthesis of Apixaban intermediate G was evaluated. A practical and efficient eight-step process was developed for the preparation of the key intermediate (G) of Apixaban starting from inexpensive 4-chloronitrobenzene and piperidine.
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