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.
Derivatives of bicyclic aminoacids agents containing these compounds and their use
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, (2008/06/13)
Disclosed are cis, exo- and trans-compounds of the formula I STR1 in which n denotes 0, 1 or 2, R1 denotes hydrogen, (C1 -C6)-alkyl which can optionally be substituted by amino, (C1 -C4)-acyl- or bezoylamino, (C2 -C6)-alkenyl, (C5 -C9)-cycloalkyl, (C5 -C9)-cycloalkenyl, (C5 -C7)-cycloalkyl-(C1 -C4)-alkyl, aryl or partially hydrogenated aryl, which can, in each case, be substituted by (C1 -C2)-alkyl, (C1 -C2)-alkoxy or halogen, aryl-(C1 -C4)-alkyl, /which can be substituted as defined previously in the aryl radical/, a monocyclic or bicyclic sulfur or nitrogen and/or nitrogen heterocyclic radical, or a side chain of naturally occurring aminoacid, R2 denotes hydrogen, (C1 -C6)-alkyl, (C2 -C6)-alkenyl or aryl-(C1 -C4)-alkyl, Y denotes hydrogen or hydroxyl, Z denotes hydrogen or Y and Z together denote oxygen, X denotes (C1 -C6)-alkyl, (C2 -C6)-alkenyl, (C6 -C9)-cycloalkyl or aryl which can be mono-, di- or tri- substituted by (C1 -C4)-alkyl, (C1 -C4)-alkoxy, hydroxyl, halogen, nitro, amino, (C1 -C4)-alkylamino, di-(C1 -C4 -alkylamino or methylenedioxy, or indol-3-yl, or physiologically acceptable salts thereof, a process of the preparation thereof, agents containing them, their use as a medicine and intermediates for the preparation thereof.
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.
