Ring Opening of Spiroepoxides Dithianedioxide with Bis-nucleophiles

Abstract

This research was aimed to apply the spiroepoxide dithianedioxide for the synthesis of amino acid via ring opening of the spiroepoxide by bis-nucleophiles. First attempt was made to synthesize the bis-nucleophiles, amino alcohol, which was eventually used to the ring opening reaction of the spiroepoxide to produce the morpholine ring compound. The reaction was carried out in racemic and asymmetric method with moderate yield and high 99%. The last step produced amino acid that was still remained unsuccessful. However, it cannot be concluded yet whether the spiroepoxide dithianedioxide is the right intermediate for the synthesis of amino acid.Keywords: Amino alcohol; Morpholine ring; Spiroepoxide dithianedioxide; Amino acid.© 2011 JSR Publications. ISSN: 2070-0237 (Print); 2070-0245 (Online). All rights reserved.doi: 10.3329/jsr.v3i3.6746 J. Sci. Res. 3 (3), 585-596 (2011)

Synthesis of curcumin derivatives containing non-steroidal anti-inflammatory drugs

“…Knoevenagel condensation took place in about 48 h. The last proposed direction of modulation of the curcumin structure was the use of its monocarbonyl analog (5). It was obtained by reacting acetone with vanillin in a 1:2 molar ratio in a hydrochloric acid medium according to a known method (37). The obtained keto-blocked substrates (2)(3)(4) were used in the next step for the synthesis of final curcumin type-NSAID derivatives.…”

“…In total, scientists have recognized curcumin as being pharmacologically effective, but unfortunately, showing many pharmacokinetic defects. The interest in designing and synthesis further curcumin analogs continues (36)(37)(38). The most frequently used possibilities for modifying the symmetrical curcumin structure are presented in Figure 1.…”

“…A wide variety of curcumin derivatives and analogs have been described in the literature (23,(36)(37)(38)(39). They include the derivatives with modifications in the aromatic rings (40), in the substituents in these rings, e.g.…”