The Production Process of 4-[(4-Methyl-1,4-dioxido-1-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]phenyl]benzamide

The Production Process of 4-[(4-Methyl-1,4-dioxido-1-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]phenyl]benzamide: An Overview

4-[(4-Methyl-1,4-dioxido-1-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]phenyl]benzamide, commonly known as MK-8628, is a pharmaceutical compound that is currently being investigated for its potential therapeutic effects on various diseases, including cancer and Alzheimer's disease.
This compound is synthesized through a complex series of chemical reactions and is typically produced in a multi-step synthesis process.
In this article, we will provide an overview of the production process of MK-8628, including the key steps involved and the chemical reactions that take place during each step.

Step 1: Synthesis of 4-[(1,4-dioxido-1-piperazinyl)methyl]benzamide
The synthesis of 4-[(1,4-dioxido-1-piperazinyl)methyl]benzamide, also known as EZ-218, is the starting material for the synthesis of MK-8628.
This compound is synthesized by reacting 4-methylphenylamine with 1,4-dioxido-1-piperazine in the presence of a Lewis acid catalyst, such as boron trifluoride diethyl ether.
The reaction occurs in a polar protic solvent, such as ethanol, and is typically carried out at a temperature of around 80-100°C.

Step 2: Synthesis of 4-[(4-Methyl-1,4-dioxido-1-piperazinyl)methyl]benzamide
Once the synthesis of 4-[(1,4-dioxido-1-piperazinyl)methyl]benzamide is complete, the next step is to further functionalize the compound.
This is achieved by reacting 4-[(1,4-dioxido-1-piperazinyl)methyl]benzamide with methyl iodide in the presence of a Lewis acid catalyst, such as zinc chloride.
The reaction occurs in a polar protic solvent, such as ethanol, and is typically carried out at a temperature of around 80-100°C.

Step 3: Synthesis of N-[4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]phenyl]-4-[(1,4-dioxido-1-piperazinyl)methyl]benzamide
In this step, the target compound, MK-8628, is synthesized by reacting N-[4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]phenyl]benzamide with 4-[(1,4-dioxido-1-piperazinyl)methyl]benzamide in the presence of a Lewis acid catalyst, such as zinc chloride.
The reaction occurs in a polar protic solvent, such as ethanol, and is typically carried out at a temperature of around 80-100°C.

Overall, the production process of MK-8628 involves a series of chemical reactions that are carried out in a multi-step synthesis process.
The key steps include the synthesis of 4-[(1,4-dioxido-1-piperazinyl)methyl]benzamide, the further functionalization of this compound with methyl iodide, and the final synthesis of the target compound, MK-8628, through the reaction of N-[4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]