Abstract
A convenient and practical synthetic route was here developed for the preparation of the cis isomer of cariprazine (2), a dopamine D3-preferring D3-D2 receptor partial agonist for the treatment of schizophrenia. The key step is the concise preparation of 2-(4-(3,3-dimethylureido)cyclohexyl)acetic acid in the cis configuration via a recrystallization separation tactic. The entire synthetic procedure was performed under mild conditions avoiding any need for expensive material, hazardous conditions, ultralow temperatures or tedious purification processes. The cis configuration of 2 confirmed via X-ray crystallography.
Graphical Abstract
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