210037-58-4Relevant articles and documents
Synthesis of BACE1 Inhibitors E2609 / E2071 via Oxime-Olefin Cycloaddition following a Process Risk Mitigation Strategy
Benayoud, Farid,Bracke, Markus,Chanda, Arani,Dimopoulos, Paschalis,Fang, Francis G.,Farthing, Christopher N.,Hall, Adrian,Ishida, Tasuku,Kaneko, Toshihiko,Kayano, Akio,Khan, Afzal,Kim, Dae-Shik,Kita, Yoichi,Lu, Lily,Mitasev, Branko,Motoki, Takafumi,Nagai, Mitsuo,Omori, Masayuki,Schnaderbeck, Matthew,Suzuki, Yuichi,Takaishi, Mamoru,Takeda, Kunitoshi,Wakasugi, Kazunori,Watanabe, Yuzo,Yamamoto, Noboru,Yoshizawa, Kazuhiro,Zhang, Huiming
, (2021/08/24)
Process development of E2609 from the preclinical stage to the clinical stage following a process risk mitigation strategy is described here. Key features include a turbo Grignard reaction monitored by in-situ IR, [3 + 2] cycloaddition in water, chemoselective amide coupling via in-situ protection, and a Reformatsky/decarboxylation approach to install a difluoromethyl group. Toward safe and scalable manufacture of E2071, an analog of E2609, a flow-reaction process for trifluoromethylation of aldehydes is presented here.
INHIBITORS OF FARNESYL-PROTEIN TRANSFERASE
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, (2008/06/13)
The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.