Diastereoselective Synthesis of 6″-(Z)- and 6″-(E)-Fluoro Analogues of Anti-hepatitis B Virus Agent Entecavir and Its Evaluation of the Activity and Toxicity Profile of the Diastereomers

Author:

Kumamoto Hiroki1,Fukano Misato1,Nakano Tomohiko1,Iwagami Keito1,Takeyama Chiaki1,Kohgo Satoru2,Imoto Shuhei3,Amano Masayuki4,Kuwata-Higashi Nobuyo4,Aoki Manabu5,Abe Hiroshi6,Mitsuya Hiroaki7,Fukuhara Kiyoshi1,Haraguchi Kazuhiro8

Affiliation:

1. School of Pharmacy, Showa University, 1-5-8 Hatanodai, Shinagawa-ku, Tokyo 142-8555, Japan

2. Center for Clinical Sciences, National Center for Global Health and Medicine, 1-21-1 Toyama, Shinjuku, Tokyo 162-8655, Japan

3. Faculty of Pharmaceutical Sciences, Sojo University, 4-22-1 Ikeda, Kumamoto 860-0082, Japan

4. Department of Infectious Diseases and Hematology, Kumamoto University School of Medicine, Kumamoto 860-8556, Japan

5. Department of Medical Technology, Kumamoto Heath Science University, 325 Izumimachi, Kumamoto 861-5598, Japan

6. Department of Chemistry, Graduate School of Science, Nagoya University, Furo-cho, Chikusa-ku, Nagoya 464-8602, Japan

7. Experimental Retrovirology Section, HIV and AIDS Malignancy Branch, National Cancer Institute, National Institutes of Health, Bethesda, Maryland 20892, United States

8. Nihon Pharmaceutical University, 10281 Komuro, Inamachi, Kita-adachi-gun, Saitama 362-0806, Japan

Funder

Japan Society for the Promotion of Science

Ministry of Health, Labour and Welfare

Publisher

American Chemical Society (ACS)

Subject

Organic Chemistry

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