A New and Practical Synthesis of Cariprazine through the Facile Construction of 2-[ trans -4-(3,3-Dimethylureido)cyclohexyl]acetic Acid

Xiaowen Chen; Feng Ni; Yu Liu; Lei Fu; Jianqi Li

doi:10.1055/s-0035-1561865

A New and Practical Synthesis of Cariprazine through the Facile Construction of 2-[ trans -4-(3,3-Dimethylureido)cyclohexyl]acetic Acid

Xiaowen Chen, Feng Ni, Yu Liu, Lei Fu^*, Jianqi Li

^*Corresponding author for this work

Research output: Contribution to journal › Article › peer-review

6 Citations (Scopus)

Abstract

A new, practical, and improved synthetic route to cariprazine is described. The key step is the facile preparation of 2-[4-(3,3-dimethylureido)cyclohexyl]acetic acid in the trans configuration through direct recrystallization. The entire synthetic procedure was accomplished under mild conditions while avoiding tedious purification processes. The trans configuration of cariprazine was confirmed by X-ray crystallographic analysis.

Original language	English
Article number	ss-2016-h0196-op
Pages (from-to)	3120-3126
Number of pages	7
Journal	Synthesis (Germany)
Volume	48
Issue number	18
DOIs	https://doi.org/10.1055/s-0035-1561865
Publication status	Published - 19 Sept 2016
Externally published	Yes

Keywords

X-ray crystallography
antipsychotic agents
cariprazine
recrystallization
synthetic methods
trans configuration

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10.1055/s-0035-1561865

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title = "A New and Practical Synthesis of Cariprazine through the Facile Construction of 2-[ trans -4-(3,3-Dimethylureido)cyclohexyl]acetic Acid",

abstract = "A new, practical, and improved synthetic route to cariprazine is described. The key step is the facile preparation of 2-[4-(3,3-dimethylureido)cyclohexyl]acetic acid in the trans configuration through direct recrystallization. The entire synthetic procedure was accomplished under mild conditions while avoiding tedious purification processes. The trans configuration of cariprazine was confirmed by X-ray crystallographic analysis.",

keywords = "X-ray crystallography, antipsychotic agents, cariprazine, recrystallization, synthetic methods, trans configuration",

author = "Xiaowen Chen and Feng Ni and Yu Liu and Lei Fu and Jianqi Li",

note = "Funding Information: This work was supported by National Natural Science Foundation of China (Grant No. 81302630), Key Technologies R&D Program of Shanghai Municipal Science and Technology Commission (Grant No. 13431900201), Natural Science Foundation of Shanghai (Grant No. 14ZR1440300), and the National Science and Technology Major Project (Grant No. 2012ZX09102101-014).",

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AU - Liu, Yu

AU - Fu, Lei

AU - Li, Jianqi

N1 - Funding Information: This work was supported by National Natural Science Foundation of China (Grant No. 81302630), Key Technologies R&D Program of Shanghai Municipal Science and Technology Commission (Grant No. 13431900201), Natural Science Foundation of Shanghai (Grant No. 14ZR1440300), and the National Science and Technology Major Project (Grant No. 2012ZX09102101-014).

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N2 - A new, practical, and improved synthetic route to cariprazine is described. The key step is the facile preparation of 2-[4-(3,3-dimethylureido)cyclohexyl]acetic acid in the trans configuration through direct recrystallization. The entire synthetic procedure was accomplished under mild conditions while avoiding tedious purification processes. The trans configuration of cariprazine was confirmed by X-ray crystallographic analysis.

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KW - antipsychotic agents

KW - cariprazine

KW - recrystallization

KW - synthetic methods

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A New and Practical Synthesis of Cariprazine through the Facile Construction of 2-[ trans -4-(3,3-Dimethylureido)cyclohexyl]acetic Acid

Abstract

Keywords

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