Boric Acid/Glycerol as an Efficient Catalyst for Synthesis of Thiomorpholine 1, 1-Dioxide by Double Michael Addition Reaction in Water

AZ Halimehjnai, S Hosseyni, H Gholami…

Index: Halimehjnai, Azim Ziyaei; Hosseyni, Seyedmorteza; Gholami, Hadi; Hashemi, Mohammed M. Synthetic Communications, 2013 , vol. 43, # 2 p. 191 - 197,7

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Abstract

Synthesis of N-substituted thiomorpholine 1,1-dioxide is the key step for the synthesis of PNU-288034 (linezolid family), which was recently targeted for clinical development. [ 1 1. (a) Brickner , SJ ; Barbachyn , MR ; Hutchinson , DK ; Manninen , PR Linezolid (ZYVOX), the first member of a completely new class of antibacterial agents for treatment of serious Gram-positive infections . J. Med. Chem. 2008 , 51 , 1981 – 1990 ; (b) Ippolito , JA ; Kanyo , ZF ; Wang , ...