A practical synthesis of deuterated methylamine and dimethylamine

Abstract

In recent years, several deuterated drugs have entered clinical trials and have been approved for use. Deuterated methylamine and dimethylamine as important intermediates play significant roles in the preparation of deuterated drugs. In this study, we have developed a new method to prepare deuterated methylamine and dimethylamine. This method employs Boc-benzylamine as the starting material and TsOCD3 as the deuterated methylation reagent. Our method gives relatively high yields and involves simple purifications, which provide a favourable supplement for the development and synthesis of deuterated drugs in the future.

Antimicrobial Activity of Curcumin and Deuterated Curcumin

“…The deuterated and its parent compound should show comparable biological activity before determining the pharmacokinetic property. Hence scientists are still interested in substituting C-H with C-D to extend the lifetime of active drugs, with improved pharmacokinetics and toxicological aspects [14][15][16][17] . Curcumin "((1E,6E)-17-bis(4-hydroxy-3methoxyphenyl) hepta-16-diene-35-dione)" is a lipophilic polyphenol present in three Indian traditional herbs "Curcuma Longa, Curcuma Wenyujin, and Curcuma Zedoaria".…”