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Both enantiomers of chiral cis-cyclohex-4-ene-1,2-dicarboxylic acid derivatives were synthesized by optical resolution of the corresponding enantiomeric mixtures by utilizing (4S)-isopropyl-1,3-thiazolidine-2-thione followed by mild aminolysis, methanolysis, and hydrolysis.

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Objective: The present study envisage a novel series of thiazole, indole and thiazolidine derivatives, namely, N-((5-Substituted-2-phenyl-1 H-indol-3-yl)methylene)-4,5,6,7-tetrahydro-5,7,-dimethylbenzo [d]thiazole-2-amine (4a-c), 2-(5-substituted-2-phenyl-1H-indol-3-yl)-3-(4,5,6,7-trimethylbenzo[d]thiazol-2-yl)-thiazolidin-4-one (5a-c) and 5-benzylidine-2-(5-substituted-2phenyl-1H-indol-3yl)-3-(4,5,6,7-tetrahydro-5,5,7-trimethylbenzo[d]thiazol-2-yl) thiazolidin-4-one (6a-c). Methods: All the newly synthesized compounds were characterized by infrared,1H,13C nuclear magnetic resonance and mass spectral data and elemental analysis and evaluated for in vitro antimicrobial activity. Results: Novel compounds N-((5-Substituted-2-phenyl-1H-indol-3-yl)methylene)-4,5,6,7-tetrahydro-5,7,-dimethylbenzo [d]thiazole-2-amine (4a-c), 2-(5-substituted-2-phenyl-1H-indol-3-yl)-3-(4,5,6,7-trimethylbenzo[d]thiazol-2-yl)-thiazolidin-4-one (5a-c) and 5-benzylidine-2-(5-substituted-2phenyl-1H-indol-3yl)-3-(4,5,6,7-tetrahydro-5,5,7-trimethyl benzo[d]thiazol-2-yl)thiazolidin-4-one (6a-c) have been made and characterized using spectral and analytical data. The results of antibacterial and antifungal activities showed that some of the synthesized compounds exhibited promising activities. Conclusion: All the newly synthesized compounds were carried out by the broth microdilution method (NCCLS. 2002) in a DMF concentration of 500, 250, 125, and 62.5 mug/ml. Gentamycin and fluconazole are used as reference standards for antibacterial and antifungal activity, respectively. The final results revealed that compounds 4b, 5b, and 6b exhibited potent antimicrobial activity when compared to the standard drugs.

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Lagunamide C is a depsipeptide natural product with low nM cytotoxicity towards numerous cancer cell lines. Synthetically, it is disconnected to a pentapeptide backbone and polyketide unit that possesses four stereogenic centers, of which two of centers are in question (C38 & 40). Our model system highlights a high-selective aldol addition via a Crimmin’s auxiliary setting the C40 ester linkage, and a non-facially selective cyclopropanation with subsequent ring opening for the installation of the C38 methyl center.

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Herein we provide full details of studies which culminated in the first total synthesis of the polyene macrolide dermostatin A, confirming our earlier stereochemical assignment. A highly convergent synthesis was developed, featuring the cyanohydrin acetonide method for polyol construction and a Stille approach to polyene introduction. The strategies and tactics developed en route should be of value for the preparation of other members of the polyene macrolide class, as well as analogs of the dermostatins.

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The present invention relates to compounds and methods which may be useful as inhibitors of HIF pathway activity for the treatment or prevention of cancer and other hypoxia-mediated diseases.

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The stereochemical outcome of the Lewis acid-mediated glycolate addition of the titanium enolates from protected N-hydroxyacetyl-4-isopropyl-1,3- thiazolidine-2-thiones to dimethyl and dibenzyl acetals depends on the hydroxyl protecting group. Particularly, the pivaloyl protected glycolate derivative provides the reluctant anti adducts in high yields and diastereomeric ratios, which can be isolated and further converted in enantiomerically pure form to beta-methoxy or beta-benzyloxy alpha-pivaloyloxy carbonyl fragments in a straightforward manner.

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The isolation, structure elucidation, and synthesis of antalid (1), a novel secondary metabolite from Polyangium sp., is described herein. The structure elucidation of 1 was performed with the aid of mass spectrometry, high field NMR experiments, and crystal structure analysis. The absolute configuration of antalid was confirmed through the Mosher ester method and ultimately by total synthesis. In addition, the biosynthetic origin of this hybrid PKS-NRPS natural product was unraveled by the in silico analysis of its biosynthetic gene cluster.

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The invention relates to a compound of formula (I) wherein A, R1 and R2 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament

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A visible-light-promoted oxo-sulfonylation of ynamides with sulfonic acids is reported, giving rise to a collection of functionalized alpha-sulfonylated amides in a straightforward manner. The reaction proceeds sequentially through a cascade of electrophilic addition and photoinduced sulfonyl radical-sustained skeleton rearrangement. The high atom economy, mild reaction conditions, and wide substrate scope comprised the merits of this synthetic transformation.

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An efficient method for the desulfurization-oxygenation of 1,3-thiazolidine-2-thiones and 1,3-oxazolidine-2-thiones using propylene oxide and employing microwave irradiation is described. This strategy of oxygenation of the thiocarbonyl group provides an attractive methodology to prepare chiral 1,3-thiazolidin-2-ones and 1,3-oxazolidin-2-ones from the corresponding precursors in good yields. Copyright

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