253128-10-8Relevant academic research and scientific papers
INTERMEDIATE FOR PREPARING ERIBULIN MESYLATE AND PROCESS FOR PREPARING THE SAME
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Paragraph 0271-0273, (2020/12/04)
The present invention relates to a process for preparing a compound of formula (6) which is an intermediate for the preparation of eribulin mesylate with high yields and high purity, and an intermediate therefor.
PROCESS FOR PREPARATION OF ERIBULIN AND INTERMEDIATES THEREOF
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Page/Page column 22, (2020/01/31)
The present application relate to a process for preparation of 4-methylene tetrahydrofuran compound of formula II, which is useful as an intermediate for the preparation of halichondrin B analogues such as eribulin and its pharmaceutically acceptable salts thereof. The present application also provide crystalline compound of formula III and crystalline compound of formula II.
MACROCYCLIZATION REACTIONS AND INTERMEDIATES USEFUL IN THE SYNTHESIS OF ANALOGS OF HALICHONDRIN B
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Page/Page column 179; 184, (2015/05/19)
The invention provides methods for the synthesis of eribulin or a pharmaceutically acceptable salt thereof (e.g., eribulin mesylate) through a macrocyclization strategy. The macrocyclization strategy of the present invention involves subjecting a non-macrocyclic intermediate to a carbon-carbon bond-forming reaction (e.g., an olefination reaction (e.g., Horner-Wadsworth-Emmons olefination), Dieckmann reaction, catalytic Ring-Closing Olefin Metathesis, or Nozaki-Hiyama-Kishi reaction) to afford a macrocyclic intermediate. The invention also provides compounds useful as intermediates in the synthesis of eribulin or a pharmaceutically acceptable salt thereof and methods for preparing the same.
Process development of halaven: Synthesis of the C14-C35 fragment via iterative nozaki-hiyama-kishi reaction-williamson ether cyclization
Austad, Brian C.,Benayoud, Farid,Calkins, Trevor L.,Campagna, Silvio,Chase, Charles E.,Choi, Hyeong-Wook,Christ, William,Costanzo, Robert,Cutter, James,Endo, Atsushi,Fang, Francis G.,Hu, Yongbo,Lewis, Bryan M.,Lewis, Michael D.,McKenna, Shawn,Noland, Thomas A.,Orr, John D.,Pesant, Marc,Schnaderbeck, Matthew J.,Wilkie, Gordon D.,Abe, Taichi,Asai, Naoki,Asai, Yumi,Kayano, Akio,Kimoto, Yuichi,Komatsu, Yuki,Kubota, Manabu,Kuroda, Hirofumi,Mizuno, Masanori,Nakamura, Taiju,Omae, Takao,Ozeki, Naoki,Suzuki, Taeko,Takigawa, Teiji,Watanabe, Tomohiro,Yoshizawa, Kazuhiro
, p. 327 - 332 (2013/04/10)
Multikilogram manufacturing process of the Halaven C14-C35 fragment is described. The synthesis features convergent assembly of subunits by iterative asymmetric Ni/Cr-mediated coupling executed in fixed equipment. Georg Thieme Verlag Stuttgart - New York.
COMPOUNDS USEFUL IN THE SYNTHESIS OF HALICHONDRIN B ANALOGS
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, (2011/08/06)
In general, the invention features compounds useful for the synthesis of analogs of halichondrin B, such as eribulin or pharmaceutically acceptable salts thereof, e.g., eribulin mesylate. Exemplary compounds are of formula (I), (II), or (III):
INTERMEDIATES FOR THE PREPARATION OF HALICHONDRIN B
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Page/Page column 85, (2010/02/15)
The present invention provides macrocyclic compounds, synthesis of the same and intermediates thereto. Such compounds, and compositions thereof, are useful for treating or preventing proliferative disorders Formula (F-4).
Macrocyclic ketone analogues of halichondrin B
Zheng, Wanjun,Seletsky, Boris M.,Palme, Monica H.,Lydon, Paul J.,Singer, Lori A.,Chase, Charles E.,Lemelin, Charles A.,Shen, Yongchun,Davis, Heather,Tremblay, Lynda,Towle, Murray J.,Salvato, Kathleen A.,Wels, Bruce F.,Aalfs, Kimberley K.,Kishi, Yoshito,Littlefield, Bruce A.,Yu, Melvin J.
, p. 5551 - 5554 (2007/10/03)
Synthesis and SAR studies of structurally simplified analogues of marine natural product halichondrin B resulted in the discovery of E7389, a new potential antitumor agent currently undergoing Phase I clinical trials. Structurally simplified macrocyclic ketone analogues of halichondrin B were prepared by total synthesis and found to retain the potent cell growth inhibitory activity in vitro, stability in mouse serum, and in vivo efficacy of the natural product.
Intermediate compounds for preparing macrocylcic analogs
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Page column 45-46, (2008/06/13)
Intermediate compounds of the formulas for use in the preparation of macrocyclic analogs.
