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2,6-Bis(chloromethyl)pyridine and 2,6-Bis(hydroxymethyl)pyridine - two valuable precursors for synthesis of macrocycles and novel drug candidates

February 17, 2023

2,6-Bis(chloromethyl)pyridine and 2,6-Bis(hydroxymethyl)pyridine are versatile heterocyclic building blocks derived from 2,6-Lutidine to be used for the synthesis of a variety of intermediates for pharmaceuticals, agrochemicals, and other specialty chemicals.  

Both compounds are considered valuable precursors in manufacturing macrocycles [1], and they have been used in the synthesis of novel drug candidates for fighting against diseases like tuberculosis [2] and cancer [3].

Pyridine derivatives

VIO Chemicals biocatalytic route to 2,6-Bis(hydroxymethyl)pyridine

We have developed a biocatalytic route that offers a simplified and cost-effective manufacturing process for 2,6-Bis(hydroxymethyl)pyridine [4]. This enzymatic transformation simplifies the multi-step classical chemical route to a one-pot reaction, offering a sustainable alternative with high productivity and excellent space-time yields.

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References:

1. M. Le Fur, O. Fougère, O. Rousseaux, (2018). Expanding the Family of Pyclen-Based Ligands Bearing Pendant Picolinate Arms for Lanthanide Complexation

in Inorg. Chem., 57,6932-45

2. V. Antoci, (2019). Bis-(imidazole/benzimidazole)-pyridine derivatives: Synthesis, structure and antimycobacterial activity, Future Medicinal Chemistry, 10.4155/fmc-2019-0063

3. Vernalis patent WO 2009156737, Synthesis of Ciforadenant

4. Vio Chemicals patent, not published yet

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