One-Pot Conversion of Benzyl Alcohols to N-Protected Anilines and Alkyl Alcohols to Carbamoyl Azides

One-pot reaction is an efficient synthesis method performing the multiple reaction sequence without isolating intermediates. We have developed a new method to synthesize protected amines from alcohols in one-pot by use of cheap and easy-to-handle trichloroisocyanuric acid and light irradiation, omitting intermediate purification steps. With this method, we synthesized memantine hydrochloride, an anti-dementia drug used worldwide. We anticipate the one-pot conversions described herein to not only provide valuable amines directly from alcohols, but provide essential building blocks and intermediates for the synthesis of bioactive molecules including drug candidates. [Open Access]