1388651-30-6Relevant 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.
FUSED AMINODIHYDROTHIAZINE DERIVATIVES
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Page/Page column 151, (2009/09/05)
A compound represented by the general formula: or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein Ring A is a C6-14 aryl group or the like, L is —NReCO— or the like (wherein Re is a hydrogen atom or the like), Ring B is a C6-14 aryl group or the like, X is a C1-3 alkylene group or the like, Y is a single bond or the like, Z is a C1-3 alkylene group or the like, R1 and R2 are each independently a hydrogen atom or the like, and R3, R4, R5 and R6 are independently a hydrogen atom, a halogen atom or the like, has an Aβ production inhibitory effect or a BACE1 inhibitory effect and is useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by Aβ and typified by Alzheimer-type dementia.