- Synthesis and application of N-3,5-dinitrobenzoyl and C3 symmetric diastereomeric chiral stationary phases
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Three diastereomeric chiral compounds, namely, (R,R)-(+)-2-amino-1,2-diphenylethanol, (1S,2R)-(+)-2-amino-1,2-diphenylethanol, and (1R,2R)-(+)-1,2-diphenylethylenediamine were used as starting materials for preparing three N-3,5-dinitrobenzoyl derivative
- Ryoo, Jae Jeong,Yu, Jeong Jae
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- Synthesis method of thioazoline-2-thioketone
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The invention discloses a synthetic method of thioazoline-2-thioketone. The synthesis method of the thioazoline-2-thioketone compound represented by a formula IV comprises the following steps: (1) ina solvent, carrying out a salt forming reaction defined in the specification on a compound represented by a formula I and chlorosulfonic acid to obtain a compound represented by a formula II; and (2)in a solvent, carrying out a cyclization reaction defined in the specification on the compound represented by the formula II and a compound represented by a formula III to obtain the thioazoline-2-thioketone compound represented by the formula IV, wherein R and R' are independently selected from hydrogen, C1-6 alkyl, C6-10 aryl substituted C1-6 alkyl and C6-10 aryl, R'' is C1-6 alkyl, and M is analkali metal. The synthesis method is simple to operate, high in yield and high in purity.
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Paragraph 0064-0066
(2020/05/29)
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- Radical-Mediated Thiol-Ene Strategy: Photoactivation of Thiol-Containing Drugs in Cancer Cells
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Photoactivated drugs provide an opportunity to improve efficacy alongside reducing side-effects in the treatment of severe diseases such as cancer. Described herein is a photoactivation decaging method of isobutylene-caged thiols through a UV-initiated thiol-ene reaction. The method was demonstrated with an isobutylene-caged cysteine, cyclic disulfide-peptide, and thiol-containing drug, all of which were rapidly and efficiently released under mild UV irradiation in the presence of thiol sources and a photoinitiator. Importantly, it is shown that the activity of histone deacetylase inhibitor largazole can be switched off when stapled, but selectively switched on within cancer cells when irradiated with non-phototoxic light.
- Sun, Shuang,Oliveira, Bruno L.,Jiménez-Osés, Gonzalo,Bernardes, Gon?alo J. L.
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supporting information
p. 15832 - 15835
(2018/11/10)
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- Total synthesis and structural validation of cyclodepsipeptides solonamide A and B
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Microorganisms are an attractive source of new natural products with antimicrobial properties, and the marine environment constitutes a prolific resource of bioactive microorganisms. During a global research expedition (Galathea III), two depsipeptides, solonamide A and solonamide B, were isolated from the marine bacterium Photobacterium halotolerance and were found to inhibit virulence gene expression in the serious human pathogen, Staphylococcus aureus. They act by interfering with the agr quorum sensing system and show resemblance to the endogenous S. aureus quorum sensing peptide, autoinducing peptide I (AIP-I). To enable more comprehensive studies, we embarked on the chemical synthesis of solonamides A and B. The key synthetic steps were formation of the (R)-β-hydroxy-fatty-acids by stereo-selective aldol reactions and a cyclative macrolactamization, which proceeded under highly dilute conditions. Thus, the first total syntheses of the solonamides corroborated the originally assigned structures, and by changing the stereochemistry of the auxiliary in the aldol steps we gained access to the natural products as well as their β3-epimers.
- Kitir, Betül,Baldry, Mara,Ingmer, Hanne,Olsen, Christian A.
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p. 7721 - 7732
(2014/12/10)
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- Stereoselective total synthesis of polyrhacitides A and B
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Two aliphatic polyketide natural products, polyrhacitides A and B, have been synthesized in a concise and highly stereoselective manner. The synthesis involved an auxiliary-based acetate aldol reaction to generate the initial stereogenic center and an ite
- Yadav,Rajendar, Goreti
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supporting information; experimental part
p. 6781 - 6788
(2011/12/21)
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