The Synthetic Routes of 4-Ethynyl-2-pyrimidinamine

4-Ethynyl-2-pyrimidinamine is a synthetic compound that has various applications in the chemical industry.
This compound is used as a building block for the synthesis of various drugs, agrochemicals, and other chemicals.
The synthesis of 4-ethynyl-2-pyrimidinamine can be achieved through several synthetic routes, some of which are outlined below.

1. The Strain-Promoted Route

The strain-promoted route is a commonly used method for the synthesis of 4-ethynyl-2-pyrimidinamine.
This method involves the use of an appropriate strain, such as p-toluenesulfonic acid, to promote the reaction between the starting materials.
The reaction typically involves the reduction of 2-chloro-4-nitro-5-phenyl-1,3-oxazolidine-3-one with a reductant such as lithium aluminum hydride or diisopropyl zinc in the presence of the strain.
The product is then isolated and purified using conventional methods.

2. The Reductive Amination Route

The reductive amination route is another commonly used method for the synthesis of 4-ethynyl-2-pyrimidinamine.
This method involves the reduction of 2-chloro-4-nitro-5-phenyl-1,3-oxazolidine-3-one with a reducing agent such as lithium aluminum hydride, hydrogen platinum, or sodium borohydride in the presence of an amine base such as methylamine, ethylamine, or propylamine.
The product is then isolated and purified using conventional methods.

3. The Reductive Nitration Route

The reductive nitration route is another method for the synthesis of 4-ethynyl-2-pyrimidinamine.
This method involves the reduction of 2-chloro-4-nitro-5-phenyl-1,3-oxazolidine-3-one with a reducing agent such as hydride, lithium aluminum hydride, or diisopropyl zinc in the presence of a nitro group as a starting material.
The product is then isolated and purified using conventional methods.

4. The Direct Reduction Route

The direct reduction route is a method for the synthesis of 4-ethynyl-2-pyrimidinamine that involves the direct reduction of 2-chloro-4-nitro-5-phenyl-1,3-oxazolidine-3-one with a reducing agent such as lithium aluminum hydride, hydrogen platinum, or sodium borohydride.
The reaction typically takes place in the presence of a solvent such as THF or DMF, and the product is isolated and purified using conventional methods.

5. The Chemical Reduction Route

The chemical reduction route is a method for the synthesis of 4-ethynyl-2-pyrimidinamine that involves the reduction of 2-chloro-4-nitro-5-phenyl-1,3-oxazolidine-3-one using a reducing agent such as hydride, lithium aluminum hydride, or diisopropyl zinc in the presence of an appropriate solvent such as acetonitrile or DMF.
The product is then isolated and purified using conventional methods.

In conclusion, the synthesis of 4-ethynyl-2-pyrimidinamine can be achieved through several synthetic routes, each of which has its own advantages and disadvantages.
The choice of a particular route depends on various factors, including the availability of starting materials, the purity of the desired product, and the cost and efficiency of the synthesis.
Regardless of the route chosen, the synthesis of 4-