Description
Aripiprazole
lauroxil is a long acting injectable (LAI) pro-drug formulation
of aripiprazole approved in the U.S. for the treatment of
schizophrenia. Aripiprazole lauroxil is a dopamine D2
receptor partial antagonist, a 5-HT2A antagonist, and a 5-
HT1A partial agonist that was developed by Alkermes. It was Aripiprazole
lauroxil is a long acting injectable (LAI) pro-drug formulation
of aripiprazole approved in the U.S. for the treatment of
schizophrenia.28 Aripiprazole lauroxil is a dopamine D2
receptor partial antagonist, a 5-HT2A antagonist, and a 5-
HT1A partial agonist that was developed by Alkermes. It was
Definition
ChEBI: A dodecanoate ester obtained by formal condensation of the carboxy group of dodecanoic acid with the hydroxy group of 7-{4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butoxy}-2-oxo-3,4-dihydroquinolin-1(2H)-yl]methanol. A prodrug for aripipraz
le, it is used for treatment of schizophrenia.
Synthesis
The synthesis of aripiprazole lauroxil has only been described
on gram scale in the patent literature. Commercially available aripiprazole (58) was
treated with formaldehyde to give hemiaminal 59 in 65% crude
yield and was then heated with lauric anhydride to give
aripiprazole lauroxil (VII) in 21% overall yield.
