Ten-Gram-Scale Total Synthesis of the Anticancer Drug Candidate E7130 to Supply Clinical Trials

E7130 is a novel drug candidate with an exceedingly complex chemical structure of the halichondrin class, discovered by a total synthesis approach through joint research between the Kishi group at Harvard University and Eisai. Only 18 months after completion of the initial milligram-scale synthesis,...

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Bibliographic Details
Published in:Organic letters 2024-04, Vol.26 (14), p.2837-2842
Main Authors: Kaburagi, Yosuke, Kira, Kazunobu, Yahata, Kenzo, Iso, Kentaro, Sato, Yuki, Matsuura, Fumiyoshi, Ohashi, Isao, Matsumoto, Yasunobu, Isomura, Minetaka, Sasaki, Takeo, Fukuyama, Takashi, Miyashita, Yusuke, Azuma, Hiroshi, Iida, Daisuke, Ishida, Tasuku, Itano, Wataru, Matsuda, Masaaki, Matsukura, Masayuki, Murai, Norio, Nagao, Satoshi, Seki, Masashi, Yamamoto, Akihiko, Yamamoto, Yuji, Yoneda, Naoki, Watanabe, Yuzo, Kamada, Atsushi, Kayano, Akio, Tagami, Katsuya, Asano, Osamu, Owa, Takashi, Kishi, Yoshito
Format: Article
Language:English
Subjects:
Antineoplastic Agents - pharmacology
Humans
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Summary:E7130 is a novel drug candidate with an exceedingly complex chemical structure of the halichondrin class, discovered by a total synthesis approach through joint research between the Kishi group at Harvard University and Eisai. Only 18 months after completion of the initial milligram-scale synthesis, ten-gram-scale synthesis of E7130 was achieved, providing the first good manufacturing practice (GMP) batch to supply clinical trials. This paper highlights the challenges in developing ten-gram-scale synthesis from the milligram-scale synthesis.
ISSN:1523-7060
1523-7052
DOI:10.1021/acs.orglett.3c03663