In
this work, we developed a catalyst-free amination of 2-mercaptobenzoxazoles
on water under microwave irradiation. The product, 2-aminobenzoxazoles,
was successfully produced via direct amination with various amines
in moderate to high yields. The formal synthesis of Suvorexant, a
medication for the treatment of insomnia, was accomplished using a
developed amination process. The reaction was completed in an hour
at 100–150 °C in a microwave reactor without the use of
external catalyst or additive. Key benefits of this process include
an on-water reaction, short reaction time, being scalable and catalyst-free,
and use of 2-mercaptobenzoxazoles as an inexpensive starting material
having low environmental impact in its preparation.
An electrochemical synthesis of 2-aminobenzoxazoles from 2-aminophenols and isothiocyanates was successfully developed in one-pot fashion. Using an inexpensive and widely available NaI and NaCl co-operatively in catalytic amounts, our electrosynthetic...
In this work, we developed a one‐pot synthesis of guanidine directly from isothiocyanate using DIB (diacetoxyiodobenzene) as a desulfurizing agent under micellar conditions in water. Our optimization study revealed that the use of 1 % TPGS‐750‐M as a surfactant with NaOH as an additive base at room temperature can convert a variety of isothiocyanates and amines into corresponding guanidines in excellent yields (69–95 %). This synthetic process in water can be applied to prepare guanidine at gram‐scale quantity. Our aqueous micellar medium also demonstrated high reusability as the reaction can be performed for several cycles without losing its efficiency. The reaction is metal‐free, utilizes water as solvent and practical (room temperature and open flask).
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