Sulfurization Efficiency in the Solution Phase Synthesis of Deoxyribonucleoside Phosphorothioates - Comparison of Sulfur Triethylamine with Various Sulfurizing Agents¹

1. Part 6 on Process Improvement Chemistry (PIC). For Part 5, refer to Ravikumar, V. T., Cheruvallath, Z. S. Bioorg. Med. Chem. Lett. (communicated).

Abstract

Efficient solution-phase synthesis of nucleoside phosphorothioates utilizing phosphoramidite approach is described. Elemental sulfur in combination with triethylamine is the prefered choice for sulfurization of phosphite triester to phosphorothioates.

1. Part 6 on Process Improvement Chemistry (PIC). For Part 5, refer to Ravikumar, V. T., Cheruvallath, Z. S. Bioorg. Med. Chem. Lett. (communicated).

Notes

1. Part 6 on Process Improvement Chemistry (PIC). For Part 5, refer to Ravikumar, V. T., Cheruvallath, Z. S. Bioorg. Med. Chem. Lett. (communicated).