Reduction O 0220Reduction of Aldehydes and Oximes to Their Corresponding Alcohols and Amines by Catalytic Hydrogenation Method. -The reduction of aldehydes and oximes to their corresponding alcohols and amines by catalytic hydrogenation is described. The reactions can also be performed on a large scale. The X-ray structure of (IIa) is reported. -(BASAPPA; DORESWAMY, B. H.; MAHENDRA, M.; MANTELINGU, K.; SRIDHAR, M. A.; PRASAD, J. S.; RANGAPPA*, K. S.; Indian J. Chem., Sect. B: Org. Chem. Incl. Med. Chem. 44 (2005) 1, 148-151; Dep. Chem., Univ. Mysore, Manasagangotri, Mysore 570 006, India; Eng.) -M. Bohle 19-056
Novel 1,5-benzothiazepin-4-(5H)-one derivatives (8a-8g) have been synthesized by intramolecular cyclization of 6 using propyl phosphonic anhydride (T3P) as a cyclodehydrating agent. The anti-angiogenic and anti-oxidant properties of the new derivatives were then evaluated. Compounds 8b, 8d, 8e, 8f and 8g exhibited very good inhibition of capillary proliferation, thus proving their anti-angiogenic properties. In addition, the in vitro antioxidant activities of these compounds were evaluated using diphenyl picryl hydrazine (DPPH), OH-, metal ion-chelating and NO (nitric oxide) assays, and the results compared with butylated hydroxytoluene (BHT), a well known anti-oxidant. Compounds 8a-8g showed excellent free-radical scavenging activities in the metal ion-chelating assay, and compounds 8f and 8g showed nitric oxide radical scavenging properties at a concentration of 20-100 µg/mL, and are thus more potent than BHT.
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