Continuous flow synthesis and scale-up of glycine-and taurine-conjugated bile salts

F Venturoni, A Gioiello, R Sardella, B Natalini…

Index: Venturoni, Francesco; Gioiello, Antimo; Sardella, Roccaldo; Natalini, Benedetto; Pellicciari, Roberto Organic and Biomolecular Chemistry, 2012 , vol. 10, # 20 p. 4109 - 4115

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Citation Number: 12

Abstract

A multi-gram scale protocol for the N-acyl amidation of bile acids with glycine and taurine has been successfully developed under continuous flow processing conditions. Selecting ursodeoxycholic acid (UDCA) as the model compound and N-ethoxycarbonyl-2-ethoxy-1, 2- dihydroquinoline (EEDQ) as the condensing agent, a modular mesoreactor assisted flow set- up was employed to significantly speed up the optimization of the reaction conditions and ...