Cariprazine, also known as RGH-188 and MP-214, is an antipsychotic drug received FDA approval on September 17, 2015. Cariprazine acts as a D2 and D3 receptor partial agonist, with high selectivity towards the D3 receptor. Action on the dopaminergic systems makes it also potentially useful as an add-on therapy in major depressive disorder. Cariprazine is approved for schizophrenia and bipolar disorder. It has also been investigated as a potential adjunct in treatment-resistant major depressive disorder.
Péter Bana, Ágnes Lakó, Nóra Zsuzsa Kiss, Zoltán Béni, Áron Szigetvári, János Kóti, György István Túrós, János Éles, and István Greiner. Synthesis of Urea Derivatives in Two Sequential Continuous-Flow Reactors. Organic Process Research & Development 2017 21 (4), 611-622. DOI: 10.1021/acs.oprd.7b00019
Shonberg J, Herenbrink CK, López L, Christopoulos A, Scammells PJ, Capuano B, Lane JR. A structure-activity analysis of biased agonism at the dopamine D2 receptor. J Med Chem. 2013 Nov 27;56(22):9199-221. doi: 10.1021/jm401318w. Epub 2013 Nov 8. PubMed PMID: 24138311.
Agai-Csongor E, Domány G, Nógrádi K, Galambos J, Vágó I, Keserű GM, Greiner I, Laszlovszky I, Gere A, Schmidt E, Kiss B, Vastag M, Tihanyi K, Sághy K, Laszy J, Gyertyán I, Zájer-Balázs M, Gémesi L, Kapás M, Szombathelyi Z. Discovery of cariprazine (RGH-188): a novel antipsychotic acting on dopamine D3/D2 receptors. Bioorg Med Chem Lett. 2012 May 15;22(10):3437-40. doi: 10.1016/j.bmcl.2012.03.104. Epub 2012 Apr 4. PubMed PMID: 22537450.
Chen, Xiaowen & Ni, Feng & Liu, Yu & fu, Lei & Li, Jianqi. (2016). A New and Practical Synthesis of Cariprazine through the Facile Construction of 2-[trans-4-(3,3-Dimethylureido)cyclohexyl]acetic Acid. Synthesis. 48. 10.1055/s-0035-1561865.
Taddei, Maurizio; Cini, Elena; Rasparini, Marcello. Process for preparation of an antipsychotic drug Cariprazine. WO 2015056164. (Assignee Chemo Research, S.L., Spain)
Agai Csongor, Eva; Czibule, Laszlo; Seboek, Ferenc; Juhasz, Balint; Galambos, Janos; Nogradi, Katalin. Process for the preparation of piperazine derivatives. WO 2010070371. (Assignee Richter Gedeon Nyrt., Hung)
Czibula, Laszlo; Juhasz, Balint; Againe Csongor, Eva; Sebok, Ferenc; Galambos, Janos; Nogradi, Katalin. Process for preparation of piperazine derivatives and hydrochloride salts thereof. WO 2011073705. (Assignee Richter Gedeon Nyrt., Hung)
Czibula, Laszlo; Juhasz, Balint; Againe Csongor, Eva; Sebok, Ferenc; Galambos, Janos; Nogradi, Katalin. Process for preparation of piperazine derivatives and hydrochloride salts thereof. WO 2011073705. (Assignee Richter Gedeon Nyrt., Hung)
Huang, Xiangchuan; Ning, Zhaolun; Wei, Genghui. Novel method for synthesizing Carpirizine. CN 108586389. (Assignee Chengdu Focus Pharmaceutical Technology Co., Ltd., Peop. Rep. China)
Cao, Longji; Sun, Li; Yang, Xiangping; Si, Chongjing; Zhang, Guisen. Process for the preparation of cariprazine. CN 106543039. (Assignee Jiangsu Nhwa Pharmaceutical Co., Ltd., Peop. Rep. China)
