Some common heterocyclic compound, 198211-38-0, name is tert-Butyl 3-azabicyclo[3.1.0]hexan-6-ylcarbamate, molecular formula is C10H18N2O2, traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc, below Introduce a new synthetic route. Safety of tert-Butyl 3-azabicyclo[3.1.0]hexan-6-ylcarbamate
General procedure: Intermediate C17.ii (130 mg) and K2C03 (69 mg) were suspended with DMF. 6-(Boc-amino)-3-azabicyclo[3. 1.0]hexane (81 mg; commercial) was added portionwise and themixture was stirred at rt for 1 day. The mixture was concentrated under reduced pressure and the residue was portioned between EA and water. The aq. layer was extracted with EA and the combined org. layers were washed with water and brine, dried over Mg504 and concentrated under reduced pressure. The title compound was obtained, after purificationby CC (Combiflash; Hept/EA 0:1 to 1:0), as a yellow oil (108 mg; 62% yield). M53 (ESI, mlz): 457.10 [M+H+]; tR = 0.73 mm.
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 198211-38-0, its application will become more common.
Reference:
Patent; ACTELION PHARMACEUTICALS LTD; CREN, Sylvaine; FRIEDLI, Astrid; RUEEDI, Georg; ZUMBRUNN, Cornelia; (200 pag.)WO2016/59097; (2016); A1;,
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