Large Scale Synthesis of an Ampakine-type Active Pharmaceutical
Ingredient Based on a Telescoped Regioselective Double Amidation Reaction
Posted on 2019-07-26 - 01:13
This
work describes the process development and manufacture of
an ampakine-type active pharmaceutical ingredient in clinical trials.
A regioselective CDI-mediated amidation process was optimized for
the subsequent couplings of two distinctive amines with a terephthalic
acid substrate. Choice of the synthetic route, key scale-up issues,
safety calorimetry, and optimization of all steps for multikilogram
production are discussed.
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Hardouin, Christophe; Pin, Frédéric; Giffard, Jean-François; Hervouet, Yvon; Hublet, Julie; Janvier, Solenn; et al. (2019). Large Scale Synthesis of an Ampakine-type Active Pharmaceutical
Ingredient Based on a Telescoped Regioselective Double Amidation Reaction. ACS Publications. Collection. https://doi.org/10.1021/acs.oprd.9b00241