87624-03-1Relevant articles and documents
Synthesis technology of 3-chloro-octahydro-2(1H)-quinolinone
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Paragraph 0026; 0027, (2016/10/31)
The invention discloses a synthesis technology of 3-chloro-octahydro-2(1H)-quinolinone. In a solvent, the 3-chloro-octahydro-2(1H)-quinolinone is used as a raw material, zinc powder and sulfuric acid are used as a reducing agent, a reaction is performed at the temperature of 0-50 DEG C for 2-6 h, a water phase is separated out, an organic phase is concentrated, a recrystallization solvent is added for stirring, and filtering and drying are performed to obtain the 3-chloro-octahydro-2(1H)-quinolinone. The synthesis technology is significantly characterized in that activation energies required by two chlorine atom reduction reactions are much different, and the reactions can be easily controlled in the single-chlorine reduction stage just by strictly controlling the reaction temperature and selecting the proper mixing solvent and the proportions thereof. Due to the fact that a series of side reactions are inhibited, the influence on the reaction time is small, and the high conversion rate is easily ensured. Due to the fact that few influence factors of the technology exist, the control conditions are mold, the technology is easily magnified, large-scale production is achieved, and guarantees on the multiple aspects of cost, quality and the like are provided for transolapril commercialized marketing.
DIASTEREOSELECTIVE SYNTHESIS OF BICYCLIC AMINO ACIDS VIA RING CONTRACTION OF α-CHLOROLACTAMS
Henning, R.,Urbach, H.
, p. 5339 - 5342 (2007/10/02)
Bicyclic lactams were converted to their α-chloro-derivatives and subjected to ring contraction under basic conditions to give bicyclic acids in diasteroselective fashion.