Application of N-Acylbenzotriazoles in the Synthesis of 5-Substituted 2-Ethoxy-1,3,4-oxadiazoles as Building Blocks toward 3,5-Disubstituted 1,3,4-Oxadiazol-2(3H)-ones

作者：Wet osot Sirawit; Phakhodee Wong; Pattarawarapan Mookda^*

来源：Journal of Organic Chemistry, 2017, 82(18): 9923-9929.

DOI：10.1021/acs.joc.7b01863

5-Substituted-2-ethox-y-1,3,4-oxadiazoks were conveniently prepared through a one-pot sequential N-acylation/dehydrative cyclization between ethyl carbazate and N-acylbenzotriazoles in the presence of Ph3P-I-2 as a dehydrating agent. Subsequent treatment with a stoichiometric amount of alkyl halides (X = Cl, Br, I) enables a rapid access to a variety of 3,5-disubstituted 1,3,4-oxadiazol-2(3H)-ones in good to excellent yields.

• 出版日期2017-9-15