Synlett 2017; 28(15): 2014-2017
DOI: 10.1055/s-0036-1588445
letter
© Georg Thieme Verlag Stuttgart · New York

A Systematic Study of the Synthesis of 2ʹ-Deoxynucleosides by Mitsunobu Reaction

Kohji Seio*
Department of Life Science and Technology, Tokyo Institute of Technology, 4259 Nagatsuta-cho Midori-ku, 226-8501, Yokohama, Japan   Email: seio.k.aa@m.titech.ac.jp
,
Munefumi Tokugawa
Department of Life Science and Technology, Tokyo Institute of Technology, 4259 Nagatsuta-cho Midori-ku, 226-8501, Yokohama, Japan   Email: seio.k.aa@m.titech.ac.jp
,
Kazuhei Kaneko
Department of Life Science and Technology, Tokyo Institute of Technology, 4259 Nagatsuta-cho Midori-ku, 226-8501, Yokohama, Japan   Email: seio.k.aa@m.titech.ac.jp
,
Takashi Shiozawa
Department of Life Science and Technology, Tokyo Institute of Technology, 4259 Nagatsuta-cho Midori-ku, 226-8501, Yokohama, Japan   Email: seio.k.aa@m.titech.ac.jp
,
Yoshiaki Masaki
Department of Life Science and Technology, Tokyo Institute of Technology, 4259 Nagatsuta-cho Midori-ku, 226-8501, Yokohama, Japan   Email: seio.k.aa@m.titech.ac.jp
› Author Affiliations
This work was supported by JSPS KAKENHI Grant Number 15H01062, 15K13738, and 26288075
Further Information

Publication History

Received: 30 March 2017

Accepted after revision: 09 May 2017

Publication Date:
07 June 2017 (online)


Abstract

The Mitsunobu reaction has emerged as an important alternative for the preparation of synthetic 2′-deoxynucleosides, which have various biological and biotechnological applications. In this work, the Mitsunobu-based synthesis of 2′-deoxynucleosides was systematically studied. The effect of phosphine, azodicarbonyl reagent, and solvent on the product yield and α/β ratio was investigated, and the highest yield and β-selectivity were obtained using (n-Bu)3P and 1,1′-(azodicarbonyl)dipiperidine in DMF. The reaction was successfully applied to various nucleobase analogues.

Supporting Information