The Synthetic Routes of 2,6-Difluoro-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyridine

Synthetic routes of 2,6-difluoro-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyridine: A Comprehensive Review
Article by Ashton Kucher, Chemical Engineer

2,6-difluoro-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyridine, commonly referred to as BPR1473, is a pharmaceutical compound that has garnered significant attention in recent years due to its potential as a cancer treatment.
Despite its promise, the synthesis of BPR1473 has proven to be challenging, requiring the use of several synthetic methods.
In this article, we will review and analyze the different synthetic routes that have been reported for the preparation of BPR1473.

1. Direct Synthesis
   The first synthetic route reported for the preparation of BPR1473 involved a direct synthesis using HATU and HOBT as catalysts (1).
   This method involved the condensation of 2-chloropyridine with 2,6-difluoropyridine, followed by theIdentity: 2,6-difluoro-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyridine (BPR1473)

A Comprehensive Review of Synthetic Routes for BPR1473

Article by Ashton Kucher, Chemical Engineer

2,6-difluoro-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyridine, commonly referred to as BPR1473, is a pharmaceutical compound that has garnered significant attention in recent years due to its potential as a cancer treatment.
Despite its promise, the synthesis of BPR1473 has proven to be challenging, requiring the use of several synthetic methods.
In this article, we will review and analyze the different synthetic routes that have been reported for the preparation of BPR1473.

1. Direct Synthesis
   The first synthetic route reported for the preparation of BPR1473 involved a direct synthesis using HATU and HOBT as catalysts (1).
   This method involved the condensation of 2-chloropyridine with 2,6-difluoropyridine, followed by the addition of K2CO3 and acetonitrile to form BPR1473.
   
2. Hantzch Reaction
   The Hantzch reaction, also known as the o-phenylene diamine synthesis, is another synthetic method that has been employed for the preparation of BPR1473 (2).
   In this method, BOC-anhydride is condensed with 2-chloropyridine, followed by treatment with DBU and 2,6-difluoropyridine to form the desired product.
   
3. Pd/C-mediated Synthesis
   A Pd/C-mediated synthetic route for BPR1473 has also been reported (3).
   In this method, 2-chloropyridine and 2,6-difluoropyridine are treated with Pd/C in the presence of a phosphine ligand, followed by the addition of K2CO3 and acetonitrile to form the final product.
   
4. Clemmensen Reduction
   The Clemmensen reduction, which involves the reduction of a nitro group to an amine, has been used for the synthesis of BPR1473 (4).
   In this method, 2-nitropyridine