29278-11-3Relevant articles and documents
Synthesis method of 2-aminoindane derivative and product of 2-aminoindane derivative
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Paragraph 0075-0077, (2017/02/24)
The invention provides a synthesis method of a 2-aminoindane derivative. According to the method, 5,6disubstituted 1-indanone is used as a staring raw material; bromination reaction is firstly performed; then, Gabriel reaction is performed; next, hydrazine hydrate is added; hydrolysis reaction is performed, and meanwhile, hydrazone is generated; finally, strong alkali is added into a high-boiling-point solvent to perform heating hydrolysis; the target product of the 2-aminoindane derivative is prepared. The invention also provides the 2-aminoindane derivative prepared by the synthesis method. Compared with the synthesis method of the 2-aminoindane derivative in the prior art, the synthesis method provided by the invention has the advantages that the reaction raw materials are cheap; the reaction condition is mild; the reaction steps are simple; the operation is easy; the yield of the obtained product is higher; the synthesis method is suitable for industrial production. Therefore good application prospects and market potentials are realized.
Halogenation of ketones with N-halosuccinimides under solvent-free reaction conditions
Pravst, Igor,Zupan, Marko,Stavber, Stojan
, p. 5191 - 5199 (2008/09/21)
Several aryl substituted ketones, cyclic ketones, 1,3-diketones and a β-ketoamide were halogenated with N-halosuccinimides under solvent-free reaction conditions (SFRC) at various temperatures (20-80 °C), whereas less enolized ketones required the presence of an acid catalyst (p-toluenesulfonic acid, PTSA). Bromination of substituted acetophenones obeys first order kinetics v=kBr[ketone] and the following correlation with the keto-enol equilibrium constant: log kBr=0.3pKE+C1, less enolized substrates being more reactive; the moderate positive charge developed in the rate determining step was confirmed by the Hammett correlation (ρ=-0.5). On the other hand, in cyclic ketones an opposite relation was observed: log kBr=-0.6pKE+C2, indicating higher reactivity of substrates with higher enolization constant (KE). The important role of the nature of the solvent (MeCN, MeOH) in preorganization of the ketone-NBS-PTSA mixture prior to SFRC bromination was found.
Improvement in the selectivity and metabolic stability of the serotonin 5-HT1A ligand, S 15535: A series of cis- and trans-2-(arylcycloalkylamine) 1-indanols
Peglion,Goument,Despaux,Charlot,Giraud,Nisole,Newman-Tancredi,Dekeyne,Bertrand,Genissel,Millan
, p. 165 - 176 (2007/10/03)
S 15535 (1) displays a distinctive profile of agonist and antagonist (weak partial agonist) activity at pre- and postsynaptic 5-HT1A receptors, respectively. It has proven to be active in several models predictive of anxiolytic, antidepressant,
