A Practical Synthesis of 3β-Amino-5-Cholestene

2013 ◽  
Vol 830 ◽  
pp. 151-154 ◽  
Author(s):  
Yue Hai You ◽  
Shan Shan Gong ◽  
Qi Sun
Keyword(s):  
Practical Method ◽  
Synthetic Route ◽  
Medicinal Value ◽  
Practical Synthesis ◽  
Derivatives Of ◽  
Substantial Interest

Derivatives of 3β-amino-5-cholestene are of substantial interest to chemical biologists and have potential medicinal value. A novel and practical method for the preparation of 3β-amino-5-cholestene from inexpensive cholesterol has been developed. To synthesize the epicholesterol intermediate, the KO2 method reported by Corey and coworkers was applied in this synthetic route and solved the problems of the known synthetic route involving epicholesterol intermediate.

Synthesis of Guanosine-Containing Dinucleoside Triphosphates

2014 ◽  
Vol 1023 ◽  
pp. 63-66
Author(s):  
Yue Hai You ◽  
Shan Shan Gong ◽  
Qi Sun
Keyword(s):  
Practical Method ◽  
Medicinal Value ◽  
Dinucleoside Polyphosphates ◽  
Substantial Interest

Dinucleoside polyphosphates have potential medicinal value and are of substantial interest to both synthetic and medicinal chemists. A practical method for the synthesis of guanosine-containing asymmetrical dinucleoside triphosphates (Gp3C and Gp3U) with 4,5-dicyanoimidazole as activator has been developed.

Practical Synthesis of β,γ-Bridging Oxygen-Modified Stavudine 5’-Triphosphates

2014 ◽  
Vol 908 ◽  
pp. 207-210
Author(s):  
Yue Hai You ◽  
Shan Shan Gong ◽  
Qi Sun
Keyword(s):  
Viral Infections ◽  
Medicinal Value ◽  
Practical Synthesis ◽  
Substantial Interest

As non-hydrolyzable analogs of stavudine 5’-triphosphate, β,γ-bridging oxygen-modified stavudine 5’-triphosphates (β,γ-CX2-NTPs, X = H, F, and Cl) possess potential medicinal value in the treatment of viral infections and are of substantial interest to both synthetic and medicinal chemists. Three β,γ-bridging oxygen-modified stavudine 5’-triphosphates were synthesized from stavudine 5’-phosphoropiperidate with 4,5-dicyanoimidazole (DCI) as the activator.

scholarly journals Practical Synthesis of 2-Iodosobenzoic Acid (IBA) without Contamination by Hazardous 2-Iodoxybenzoic Acid (IBX) under Mild Conditions

Molecules ◽  
2021 ◽  
Vol 26 (7) ◽  
pp. 1897
Author(s):  
Hideyasu China ◽  
Nami Kageyama ◽  
Hotaka Yatabe ◽  
Naoko Takenaga ◽  
Toshifumi Dohi
Keyword(s):  
Aqueous Solution ◽  
Room Temperature ◽  
Practical Method ◽  
Hypervalent Iodine ◽  
Mild Conditions ◽  
Sequential Procedures ◽  
Iodine Compounds ◽  
Practical Synthesis ◽  
Iodosobenzoic Acid ◽  
Lower Temperature

We report a convenient and practical method for the preparation of nonexplosive cyclic hypervalent iodine(III) oxidants as efficient organocatalysts and reagents for various reactions using Oxone® in aqueous solution under mild conditions at room temperature. The thus obtained 2-iodosobenzoic acids (IBAs) could be used as precursors of other cyclic organoiodine(III) derivatives by the solvolytic derivatization of the hydroxy group under mild conditions of 80 °C or lower temperature. These sequential procedures are highly reliable to selectively afford cyclic hypervalent iodine compounds in excellent yields without contamination by hazardous pentavalent iodine(III) compound.

scholarly journals Identification of pigments in artworks by inverse tangent derivative of spectrum and a new filtering method

2020 ◽  
Vol 8 (1) ◽  
Author(s):  
F. Fazlali ◽  
S. Gorji Kandi
Keyword(s):  
Reflectance Spectrum ◽  
Practical Method ◽  
Chemical Methods ◽  
Munk Function ◽  
Absorption Of Light ◽  
Spectrophotometric Data ◽  
First Time ◽  
Non Destructive ◽  
Derivatives Of

Abstract Employing an economical and non-destructive method for identifying pigments utilized in artworks is a significant aspect for preserving their antiquity value. One of the non-destructive methods for this purpose is spectrophotometry, which is based on the selected absorption of light. Mathematical descriptive methods such as derivatives of the reflectance spectrum, the Kubelka–Munk function and logarithm have been employed for the characterization of the peak features corresponding to the spectrophotometric data. In the present study, the mentioned mathematical descriptive methods were investigated with the aim to characterize the constituents of an Iranian artwork but were not efficient for the samples. Therefore, inverse tangent derivative equation was developed on spectral data for the first time, providing considerable details in the profile of reflectance curves. In the next part, to have a simpler and more practical method it was suggested to use filters made up of pure pigments. By using these filters and placing them on the samples, imaging was done. Then, images of samples with and without filter were evaluated and pure pigments were distinguished. The mentioned methods were also used to identify pigments in a modern Iranian painting specimen. The results confirmed these methods with reliable answers indicating that physical methods (alongside chemical methods) can also be effective in determining the types of pigments.

A Synthetic Route to Epoxyalkyl β-Laminaribiosides, Especially Suitable for Radiolabeling

1994 ◽  
Vol 47 (9) ◽  
pp. 1805 ◽  
Author(s):  
WM Best ◽  
RV Stick ◽  
DMG Tilbrook
Keyword(s):  
Synthetic Route ◽  
Benzyl Ethers ◽  
Derivatives Of

The major products in the controlled benzylation (NaH/PhCH2Cl) of allyl and but-3-enyl β-D-glucopyranosides were the 2,4,6-tri-O-benzyl ethers. Subsequent glycosidations of these tribenzyl ethers gave derivatives of allyl and but-3-enyl β- laminaribioside, the latter being subsequently transformed into 3,4-epoxybutyl β- laminaribioside.

scholarly journals α,ß-Didehydrosuberoylanilide hydroxamic acid (DDSAHA) as precursor and possible analogue of the anticancer drug SAHA

2019 ◽  
Vol 15 ◽  
pp. 2524-2533 ◽  
Author(s):  
Shital K Chattopadhyay ◽  
Subhankar Ghosh ◽  
Sarita Sarkar ◽  
Kakali Bhadra
Keyword(s):  
Anticancer Drug ◽  
Hela Cells ◽  
Hydroxamic Acid ◽  
Suberoylanilide Hydroxamic Acid ◽  
Oxygen Species ◽  
Synthetic Route ◽  
Metathesis Reaction ◽  
Cross Metathesis ◽  
Terminal Alkene ◽  
Derivatives Of

An alternate synthetic route to the important anticancer drug suberoylanilide hydroxamic acid (SAHA) from its α,ß-didehydro derivative is described. The didehydro derivative is obtained through a cross metathesis reaction between a suitable terminal alkene and N-benzyloxyacrylamide. Some of the didehydro derivatives of SAHA were preliminarily evaluated for anticancer activity towards HeLa cells. The administration of the analogues caused a significant decrease in the proliferation of HeLa cells. Furthermore, one of the analogues showed a maximum cytotoxicity with a minimum GI50 value of 2.5 µg/mL and the generation of reactive oxygen species (ROS) as some apoptotic features.

scholarly journals A practical synthesis of amino limonin/deoxylimonin derivatives as effective mitigators against inflammation and nociception

2020 ◽  
Vol 11 (7) ◽  
pp. 843-847
Author(s):  
Shaochi Wang ◽  
Xueqing Han ◽  
Yun Yang ◽  
Rui Chen ◽  
Zhaoyi Guo ◽  
...  
Keyword(s):  
Synthetic Route ◽  
Practical Synthesis ◽  
Amino Derivatives

A practical synthetic route, consisting of 5 steps, has been developed and applied successfully for converting limonin/deoxylimonin into the corresponding amino derivatives I-5a–I-5e and II-5a–II-5e.

scholarly journals Practical Synthesis of Precursors of Cyclohexyne and 1,2-Cyclohexadiene

Synthesis ◽  
2019 ◽  
Vol 51 (07) ◽  
pp. 1561-1564 ◽  
Author(s):  
Kentaro Okano ◽  
Ryo Nakura ◽  
Kazuki Inoue ◽  
Atsunori Mori
Keyword(s):  
Room Temperature ◽  
Practical Method ◽  
Enol Ether ◽  
One Pot ◽  
Subsequent Formation ◽  
Silyl Group ◽  
Stoichiometric Amount ◽  
Lithium Enolate ◽  
Silyl Enol Ether ◽  
Practical Synthesis

This study investigated a practical method for regiocontrolled synthesis of precursors of strained cyclohexynes and 1,2-cyclohexadienes, which is a one-pot procedure consisting of a rearrangement of silyl enol ether and subsequent formation of the enol triflates. Triethylsilyl enol ether, derived from cyclohexanone, was treated with a combination of LDA and t-BuOK in n-hexane/THF to encourage the migration of the silyl group to generate an α-silyl enolate. Subsequently, the α-silyl enolate was reacted with Comins’ reagent to yield the corresponding enol triflate. Finally, the α-silylated trisubstituted lithium enolate for the synthesis of 1,2-cyclohexadiene precursor was isomerized in the presence of a stoichiometric amount of water for one hour at room temperature to exclusively provide tetrasubstituted lithium enolate for the synthesis of cyclohexyne precursor in one pot.

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