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2-(Morpholin-4-ylamino)pyridine-5-boronic acid pinacol ester is an important intermediate in the synthesis of various pharmaceuticals, agrochemicals, and other chemicals.
It is commonly used as an intermediate in the synthesis of HIV protease inhibitors, which are widely used in the treatment of HIV infection.
The synthetic routes of 2-(morpholin-4-ylamino)pyridine-5-boronic acid pinacol ester have been extensively studied in recent years, and various methods have been developed for its synthesis.
One of the most commonly used synthetic routes for 2-(morpholin-4-ylamino)pyridine-5-boronic acid pinacol ester involves the use of boronic acid pinacol ester as a starting material.
Boronic acid pinacol ester is synthesized by the reaction of boric acid with pinacol in the presence of a catalyst, such as trimethyl orthoformate.
The reaction is exothermic, and care should be taken to maintain a safe distance from the reaction mixture.
The product is then treated with an excess of morpholine and sodium hydroxide to form the desired boronic acid pinacol ester.
Another synthetic route involves the use of 2-chloropyridine as a starting material.
2-chloropyridine is synthesized by the reaction of pyridine with chloroform in the presence of a catalyst, such as hydrochloric acid.
The resulting 2-chloropyridine is then treated with boric acid and pinacol in the presence of a catalyst, such as sodium hydroxide, to form the desired boronic acid pinacol ester.
A third synthetic route involves the use of 2-bromopyridine as a starting material.
2-bromopyridine is synthesized by the reaction of pyridine with bromoform in the presence of a catalyst, such as hydrogen bromide.
The resulting 2-bromopyridine is then treated with boric acid and pinacol in the presence of a catalyst, such as sodium hydroxide, to form the desired boronic acid pinacol ester.
Overall, the synthetic routes of 2-(morpholin-4-ylamino)pyridine-5-boronic acid pinacol ester involve the use of various starting materials and catalysts, and the choice of synthetic route depends on the availability of the starting materials and the desired yield and purity of the product.
The synthetic routes can be simplified or modified depending on the specific requirements of the synthesis.
