Copper Catalyst One-Pot Synthesis for Vortioxetine
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
The high cost of palladium catalysts limits the industrial application of existing synthetic routes for Vortioxetine, necessitating a more cost-effective and efficient method for its production.
Innovation Solution
A one-pot reaction process using a catalytic system consisting of a copper salt and an organic ligand to form both C—S and C—N bonds, providing a cheaper and industrially viable synthetic route for Vortioxetine.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If palladium catalysts are used to form C-S and C-N bonds in the synthesis of Vortioxetine, then the synthesis can be achieved with established methodology, but the production cost becomes excessively high
Solution Approach 1:
The patent replaces expensive palladium catalysts with cheaper copper catalysts that can be used in stoichiometric or near-stoichiometric amounts. The copper catalyst system, while less expensive than palladium, achieves comparable synthetic results through a one-pot double coupling approach, significantly reducing production costs while maintaining synthesis reliability
Solution Approach 2:
The patent changes the catalytic system parameters from palladium-based to copper-based catalysts, and modifies the reaction conditions to enable a one-pot double coupling process. This parameter change allows the use of cheaper copper catalysts while achieving the desired C-S and C-N bond formation through a streamlined synthetic pathway
2Manufacturing precision
If multiple separate steps are used to form C-S and C-N bonds, then each bond formation can be optimized independently, but the overall production time and complexity increase
Solution Approach 1:
The patent merges the formation of C-S and C-N bonds into a single one-pot reaction process using copper catalysts. This combining of multiple bond-forming steps into one operation reduces the overall number of steps, simplifies the synthetic process, and decreases production time while maintaining the precision of bond formation through optimized copper catalysis
Solution Approach 2:
The copper catalyst system demonstrated in the patent exhibits multi-functionality by facilitating both C-S bond formation and C-N bond formation within the same reaction pot. This universal catalytic approach eliminates the need for separate optimized steps for each bond type, reducing process complexity while maintaining manufacturing precision
Applied Scientific Principles
This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.
Function Achieved in This Case
This process achieves higher yields of Vortioxetine while reducing production costs, making it a more economically viable option for industrial-scale manufacturing.
Implementation Method 1
using a catalytic system consisting of a copper salt and an organic ligand, which can promote the formation of both C—N and C—S bond in one-pot
Implementation Method 2
using a catalytic system consisting of a copper salt and an organic ligand, which can promote the formation of both C—N and C—S bond in one-pot
Data Source
AI summary
The present invention relates to a process for the synthesis of Vortioxetine (I) or a pharmaceutically acceptable salt thereof. This process is accomplished by using a catalytic system consisting of a copper salt and an organic ligand, which can promote the formation of both C—N and C—S bond in one-pot, giving rise to an efficient, simple and industrially viable synthetic route for Vortioxetine.