1276666-10-4Relevant academic research and scientific papers
A [2 - [(5 - chloro - benzo oxazole - 2 - yl) (3 - oxo-butyl) amino] ethyl] carbamic acid tert-butyl preparation method (by machine translation)
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, (2017/04/19)
The invention discloses a [2 - [(5 - chloro - benzo oxazole - 2 - yl) (3 - oxo-butyl) amino] ethyl] carbamic acid tert-butyl preparation method, in order to ethylenediamine, vinyl, 2 - amino - 4 - chlorophenol and the like as raw materials, after five-step reaction to obtain the target product [2 - [(5 - chloro - benzo oxazole - 2 - yl) (3 - oxo-butyl) amino] ethyl] tert-butyl carbamate. The invention has simple operation, environment friendly, comprehensive yield is 52% more, than the existing 35.6% yield, with a remarkable enhancement, greatly reduces the production cost of the existing drugs, is suitable for industrial scale production. (by machine translation)
A su Wolei lives is an important intermediate for preparing method (by machine translation)
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, (2017/07/12)
The invention belongs to the field of medical technology, claims an important intermediate {2 - [(5 - chlorobenzene benzene and oxazole -2 yl) - (3 - keto - butyl) - amino] ethyl} - carbamic acid tert-butyl preparation method. The use of the toxicity is relatively small compound in place of the two connecting methyl ketene, the DBU, LDA, NaHMDS, KHMDS catalytic reaction such as, can in order to 90% high yield of the above formula (3) compound, and the HPLC of the crude product content of 99.5% or more, the method of the invention is suitable for industrial production. (by machine translation)
Process for the preparation of an intermediate for an orexin receptor antagonist
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Page/Page column 9; 10, (2017/02/02)
The present invention is directed to processes for preparing an intermediate for a diazepane compound which is an antagonist of orexin receptors, and which is useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved.
PROCESS FOR THE PREPARATION OF SUVOREXANT AND INTERMEDIATES USEFUL IN THE SYNTHESIS OF SUVOREXANT
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, (2016/07/05)
A novel processes for the preparation of suvorexant (formula I), its related compounds and its intermediates that are simple, economical and commercially viable. (I)
PROCESS FOR THE PREPARATION OF AN OREXIN RECEPTOR ANTAGONIST
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Page/Page column 38-39, (2012/11/13)
The present invention is directed to processes for preparing a diazepane compound which is an antagonist of orexin receptors, and which is useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is further directed to crystalline forms of this diazepane compound and pharmaceutical compositions thereof.
The first large-scale synthesis of MK-4305: A dual orexin receptor antagonist for the treatment of sleep disorder
Baxter, Carl A.,Cleator, Ed,Brands, Karel M. J.,Edwards, John S.,Reamer, Robert A.,Sheen, Faye J.,Stewart, Gavin W.,Strotman, Neil A.,Wallace, Debra J.
, p. 367 - 375 (2012/05/19)
A new synthetic route to drug candidate 1, a potent and selective dual orexin antagonist for the treatment of sleep disorders, has been developed. The key acyclic precursor 10 was prepared in a one-step process in 75% isolated yield from commercially available starting materials using novel chemistry to synthesize 2-substituted benzoxazoles. A reductive amination was followed by a classical resolution to afford chiral diazepane (R)-11. Finally, coupling of (R)-11 with acid 5 furnished the desired drug candidate 1.
