Tag: 200-300

Applied Enantioselective Aminocatalysis: α-Heteroatom Functionalization Reactions on the Carbapenem (β-Lactam Antibiotic) Core was written by Cele, Zamani E. D.;Arvidsson, Per I.;Kruger, Hendrik G.;Govender, Thavendran;Naicker, Tricia. And the article was included in European Journal of Organic Chemistry in 2015.Product Details of 14204-27-4 This article mentions the following:

The carbapenem (β-lactam antibiotic) scaffold serves as a useful nucleophile in organocatalytic diarylprolinol trimethylsilyl ether mediated α-heterofunctionalization reactions leading to the formation of diverse products that bear multiple stereocenters in high diastereoselectivity and moderate to good yields. Under optimized conditions the synthesis of the target compounds was achieved using (2S)-2-[diphenyl[(trimethylsilyl)oxy]methyl]pyrrolidine (chiral prolinol-silyl ether) as a catalyst. Starting materials included (5R,6S)-6-[(1R)-1-hydroxyethyl]-3,7-dioxo-1-azabicyclo[3.2.0]heptane-2-carboxylic acid (4-nitrophenyl)methyl ester, 1,2-diazenedicarboxylic acid, 1,2-bis(1,1-dimethylethyl) ester, N-(hydroxy)carbamic acid ester, (nitros)benzene,2-(phenylthio)-1H-isoindole-1,3(2H)-dione, 2-(phenylseleno)-1H-i-Isoindole-1,3(2H)-dione. In the experiment, the researchers used many compounds, for example, 2-(Phenylthio)isoindoline-1,3-dione (cas: 14204-27-4Product Details of 14204-27-4).

2-(Phenylthio)isoindoline-1,3-dione (cas: 14204-27-4) belongs to indole derivatives. Indole produced by Proteus, Pseudomonas, Escherichia and other species was shown to be a growth promoting factor in Arabidopsis thaliana. More than 200 indole derivatives have already been marketed as drugs or are under advanced stages of clinical trials.Product Details of 14204-27-4

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Synthesis and in-vitro anticancer activity of 3,5-bis(indolyl)-1,2,4-thiadiazoles was written by Kumar, Dalip;Kumar, N. Maruthi;Chang, Kuei-Hua;Gupta, Ritika;Shah, Kavita. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2011.Computed Properties of C9H5BrN2 This article mentions the following:

A series of 3,5-bis(indolyl)-1,2,4-thiadiazoles were synthesized and evaluated for their cytotoxicity against selected human cancer cell lines. Indole-3-thiocarboxamides, e.g., I, reacted with iodobenzene diacetate via oxidative dimerization to give 3,5-bis(indolyl)-1,2,4-thiadiazoles, e.g., II. Among the synthesized bis(indolyl)-1,2,4-thiadiazoles, the compound II with 4-chlorobenzyl and methoxy substituents showed the most potent activity. In the experiment, the researchers used many compounds, for example, 5-Bromo-3-cyanoindole (cas: 90271-86-6Computed Properties of C9H5BrN2).

5-Bromo-3-cyanoindole (cas: 90271-86-6) belongs to indole derivatives. Indole, also called Benzopyrrole, a heterocyclic organic compound occurring in some flower oils, such as jasmine and orange blossom, in coal tar, and in fecal matter. In addition to indole, the strain-release chemistry worked for numerous substrates including amines, alcohols, thiols, carboxylic acids, imidazoles, and pyrazoles.Computed Properties of C9H5BrN2

Referemce:
Indole alkaloid derivatives as building blocks of natural products from聽Bacillus thuringiensis聽and聽Bacillus velezensis聽and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Oxidative cleavage reaction of substituted indoles catalyzed by plant cell cultures was written by Takemoto, Masumi;Iwakiri, Yasutaka;Tanaka, Kiyoshi. And the article was included in Heterocycles in 2007.Application of 4583-55-5 This article mentions the following:

We have developed a novel method for the oxidative cleavage of indole carbon double bonds in the presence of H₂O₂ using plant cell cultures as peroxidase. The oxidative method has some advantage, as features such as mild reactions, good yields, easy work-up, and safety. In the experiment, the researchers used many compounds, for example, 5-Bromo-2,3-dimethyl-1H-indole (cas: 4583-55-5Application of 4583-55-5).

5-Bromo-2,3-dimethyl-1H-indole (cas: 4583-55-5) belongs to indole derivatives. Indole, also called Benzopyrrole, a heterocyclic organic compound occurring in some flower oils, such as jasmine and orange blossom, in coal tar, and in fecal matter.Indole was synthesized in moderate yield via an o-naphthoquinone catalyzed tandem cross-coupling of substituted aniline and benzylamine under aerobic oxidation conditions.Application of 4583-55-5

Referemce:
Indole alkaloid derivatives as building blocks of natural products from聽Bacillus thuringiensis聽and聽Bacillus velezensis聽and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Selective halogen-lithium exchange in bromophenylalkyl halides was written by Parham, William E.;Jones, Lawrence D.;Sayed, Yousry A.. And the article was included in Journal of Organic Chemistry in 1976.Reference of 5388-42-1 This article mentions the following:

Exchange of the aryl halide atom in o-BrC6H4CH2Cl, o-BrC6H4(CH2)2Br, and o-BrC6H4(CH2)3Cl for Li was carried out with BuLi in THF-hexane at -100掳. The stable lithio derivatives reacted with a variety of electrophiles; e.g., o-LiC6H4CH2Cl (I) with H2O, cyclohexanone, or PhNCO at low temperature gave, resp., PhCH2Cl, II, and III. I with H2O at room temperature gave 9,10-dihydroanthracene (not benzocyclopropene). Benzocyclobutene was formed from o-LiC6H4(CH2)2Br under similar conditions. O-halobenzyl bromides were lithiated at the benzyl bromine atom and underwent subsequent coupling to bibenzyl. O-BrC6H4(CH2)3Br with BuLi underwent intramol. coupling to indan. In the experiment, the researchers used many compounds, for example, 2-Phenylisoindolin-1-one (cas: 5388-42-1Reference of 5388-42-1).

2-Phenylisoindolin-1-one (cas: 5388-42-1) belongs to indole derivatives. Indole, also called Benzopyrrole, a heterocyclic organic compound occurring in some flower oils, such as jasmine and orange blossom, in coal tar, and in fecal matter. In addition to indole, the strain-release chemistry worked for numerous substrates including amines, alcohols, thiols, carboxylic acids, imidazoles, and pyrazoles.Reference of 5388-42-1

Referemce:
Indole alkaloid derivatives as building blocks of natural products from聽Bacillus thuringiensis聽and聽Bacillus velezensis聽and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Asymmetric sulfenylation of 3-CF₃-Oxindoles through organocatalysis with a quinidine derivative was written by E, Yidan;Yuan, Teng;Yin, Liang;Xu, Youjun. And the article was included in Tetrahedron Letters in 2017.Synthetic Route of C14H9NO2S This article mentions the following:

An asym. sulfenylation of 3-CF₃-oxindoles catalyzed by a quinidine derivative was described. 3-CF₃-oxindoles with electro-donating groups led to corresponding products in good yield and with good enantioselectivity while 3-CF₃-oxindoles bearing electro-withdrawing groups were not competent substrates due to its significant decomposition at the optimal reaction conditions. As for the sulfenylation reagents based on thiophenol, both electro-donating groups and electro-withdrawing groups were well tolerated. In the experiment, the researchers used many compounds, for example, 2-(Phenylthio)isoindoline-1,3-dione (cas: 14204-27-4Synthetic Route of C14H9NO2S).

2-(Phenylthio)isoindoline-1,3-dione (cas: 14204-27-4) belongs to indole derivatives. Indole exists overwhelmingly in the 1H-indole form as do other simple indoles. Indole plays a fundamental role for QS in E. coli, being one of the signal molecules responsible for the transcription of a variety of genes (gabT, and tnaB ASTD). Synthetic Route of C14H9NO2S

Referemce:
Indole alkaloid derivatives as building blocks of natural products from聽Bacillus thuringiensis聽and聽Bacillus velezensis聽and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Cyanine dye labeling reagents: Sulfoindocyanine succinimidyl esters was written by Mujumdar, Ratnakar B.;Ernst, Lauren A.;Mujumdar, Swati R.;Lewis, Christopher J.;Waggoner, Alan S.. And the article was included in Bioconjugate Chemistry in 1993.Computed Properties of C13H17NO3S This article mentions the following:

The synthesis and properties of a series of new fluorescent labeling reagents based on sulfoindocyanine dyes are described. They contain succinimidyl ester reactive groups and can be readily conjugated to antibodies, avidin, DNA, lipids, polymers, and other amino-group-containing materials. The labeling reagents are water soluble, pH insensitive, and show much reduced dye aggregation under labeling conditions. One of the reagents, Cy3, can be excited with the 488-, 514-, and 532-nm laser lines and is optimally excited with the 546-nm mercury arc line. Another, Cy5, can be excited with the 633-nm HeNe and 647-nm Kr laser lines available with many flow cytometers and confocal laser-scanning microscopes. New laser diodes emitting near 650 nm should also be excellent excitation sources for Cy5. In the experiment, the researchers used many compounds, for example, 1-Ethyl-2,3,3-trimethyl-3H-indol-1-ium-5-sulfonate (cas: 146368-07-2Computed Properties of C13H17NO3S).

1-Ethyl-2,3,3-trimethyl-3H-indol-1-ium-5-sulfonate (cas: 146368-07-2) belongs to indole derivatives. Indole exists overwhelmingly in the 1H-indole form as do other simple indoles.Indole was synthesized in moderate yield via an o-naphthoquinone catalyzed tandem cross-coupling of substituted aniline and benzylamine under aerobic oxidation conditions.Computed Properties of C13H17NO3S

Referemce:
Indole alkaloid derivatives as building blocks of natural products from聽Bacillus thuringiensis聽and聽Bacillus velezensis聽and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Parameterization of Acyclic Diaminocarbene Ligands Applied to a Gold(I)-Catalyzed Enantioselective Tandem Rearrangement/Cyclization was written by Niemeyer, Zachary L.;Pindi, Suresh;Khrakovsky, Dimitri A.;Kuzniewski, Christian N.;Hong, Cynthia M.;Joyce, Leo A.;Sigman, Matthew S.;Toste, F. Dean. And the article was included in Journal of the American Chemical Society in 2017.Formula: C10H8ClNO2 This article mentions the following:

Computed descriptors for acyclic diaminocarbene ligands are developed in the context of a gold catalyzed enantioselective tandem [3,3]-sigmatropic rearrangement-[2+2]-cyclization. Surrogate structures enable the rapid identification of parameters that reveal mechanistic characteristics. The observed selectivity trends are validated in a robust multivariate anal. facilitating the development of a highly enantioselective process. In the experiment, the researchers used many compounds, for example, 2-(5-Chloro-1H-indol-3-yl)acetic acid (cas: 1912-45-4Formula: C10H8ClNO2).

2-(5-Chloro-1H-indol-3-yl)acetic acid (cas: 1912-45-4) belongs to indole derivatives. Indole produced by Proteus, Pseudomonas, Escherichia and other species was shown to be a growth promoting factor in Arabidopsis thaliana. Due to this activity, the indole ring system has become an important component or intermediate in the synthesis of heterocycles.Formula: C10H8ClNO2

Referemce:
Indole alkaloid derivatives as building blocks of natural products from聽Bacillus thuringiensis聽and聽Bacillus velezensis聽and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Synthesis of a new near-IR fluorescent reagent and study on its in-situ dimer’s interaction with DNA was written by Zheng, Hong;Li, Dong-Hui;Wu, Min;Chen, Qiu-Ying;Xu, Jin-Gou. And the article was included in Gaodeng Xuexiao Huaxue Xuebao in 1999.Reference of 146368-07-2 This article mentions the following:

A new anionic Near-IR fluorescent cyanine dye was synthesized and its absorption and fluorescence spectra in water and in the solution of cationic surfactant-hexadecyltrimethyl-ammonium bromide (CTAB) were studied. The results showed that the maximum excitation wavelength and emission wavelength were 765 nm and 795 nm in water, resp. In the presence of low concentration of CTAB, the dye formed ionic associate with CTAB was made higher to form the pre-micellar aggregation, the fluorescence intensity decreased dramatically because of forming a low-fluorescent in-situ dimeric dye. When the concentration of CTAB was above the critical micelle concentration (cmc), the dimeric dye dissociated, and the fluorescence intensity of Near-IR cyanine was restored, and the maximum emission wavelength was bathochromated from 795 nm to 812 nm. The possibility of using low-fluorescent in-situ dimeric dye as a Near-IR region fluorescent probe for DNA was also studied. In the experiment, the researchers used many compounds, for example, 1-Ethyl-2,3,3-trimethyl-3H-indol-1-ium-5-sulfonate (cas: 146368-07-2Reference of 146368-07-2).

1-Ethyl-2,3,3-trimethyl-3H-indol-1-ium-5-sulfonate (cas: 146368-07-2) belongs to indole derivatives. Indole, also called Benzopyrrole, a heterocyclic organic compound occurring in some flower oils, such as jasmine and orange blossom, in coal tar, and in fecal matter. It is used in perfumery and in making tryptophan, an essential amino acid, and indoleacetic acid (heteroauxin), a hormone that promotes the development of roots in plant cuttings.Reference of 146368-07-2

Referemce:
Indole alkaloid derivatives as building blocks of natural products from聽Bacillus thuringiensis聽and聽Bacillus velezensis聽and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Photoactive electron donor-acceptor complex platform for Ni-mediated C(sp³)-C(sp²) bond formation was written by Kammer, Lisa Marie;Badir, Shorouk O.;Hu, Ren-Ming;Molander, Gary A.. And the article was included in Chemical Science in 2021.Recommanded Product: 14204-27-4 This article mentions the following:

A dual photochem./nickel-mediated decarboxylative strategy for the assembly of C(sp₃)-C(sp₂) linkages was disclosed. Under light irradiation at 390 nm, com. available and inexpensive Hantzsch ester (HE) functions as a potent organic photoreductant to deliver catalytically active Ni(0) species through single-electron transfer (SET) manifolds. As part of its dual role, the Hantzsch ester effects a decarboxylative-based radical generation through electron donor-acceptor (EDA) complex activation. This homogeneous, net-reductive platform bypasses the need for exogenous photocatalysts, stoichiometric metal reductants, and additives. Under this cross-electrophile paradigm, the coupling of diverse C(sp₃)-centered radical architectures (including primary, secondary, stabilized benzylic, 伪-oxy, and 伪-amino systems) with (hetero)aryl bromides was accomplished. The protocol proceeded under mild reaction conditions in the presence of sensitive functional groups and pharmaceutically relevant cores. In the experiment, the researchers used many compounds, for example, 2-(Phenylthio)isoindoline-1,3-dione (cas: 14204-27-4Recommanded Product: 14204-27-4).

2-(Phenylthio)isoindoline-1,3-dione (cas: 14204-27-4) belongs to indole derivatives. Indole exists overwhelmingly in the 1H-indole form as do other simple indoles. In addition to indole, the strain-release chemistry worked for numerous substrates including amines, alcohols, thiols, carboxylic acids, imidazoles, and pyrazoles.Recommanded Product: 14204-27-4

Referemce:
Indole alkaloid derivatives as building blocks of natural products from聽Bacillus thuringiensis聽and聽Bacillus velezensis聽and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Pyrazolopyrimide library screening in glioma cells discovers highly potent antiproliferative leads that target the PI3K/mTOR pathway was written by Valero, Teresa;Baillache, Daniel J.;Fraser, Craig;Myers, Samuel H.;Unciti-Broceta, Asier. And the article was included in Bioorganic & Medicinal Chemistry in 2020.Recommanded Product: 7-Azaindole-5-boronic Acid Pinacol Ester This article mentions the following:

The search for novel targeted inhibitors active on glioblastoma multiforme is crucial to develop new treatments for this unmet clin. need. Herein, we report the results from a screening campaign against glioma cell lines using a proprietary library of 100 structurally-related pyrazolopyrimidines. Data anal. identified a family of compounds featuring a 2-amino-1,3-benzoxazole moiety (eCF309 to eCF334) for their antiproliferative properties in the nM range. These results were validated in patient-derived glioma cells. Available kinase inhibition profile pointed to blockade of the PI3K/mTOR pathway as being responsible for the potent activity of the hits. Combination studies demonstrated synergistic activity by inhibiting both PI3Ks and mTOR with selective inhibitors. Based on the structure activity relationships identified in this study, five new derivatives were synthesized and tested, which exhibited potent activity against glioma cells but not superior to the dual PI3K/mTOR inhibitor and lead compound of the screening eCF324. In the experiment, the researchers used many compounds, for example, 7-Azaindole-5-boronic Acid Pinacol Ester (cas: 754214-56-7Recommanded Product: 7-Azaindole-5-boronic Acid Pinacol Ester).

7-Azaindole-5-boronic Acid Pinacol Ester (cas: 754214-56-7) belongs to indole derivatives. In addition to tryptophan, indigo, and indoleacetic acid, numerous compounds obtainable from plant or animal sources contain the indole molecular structure.Indole was synthesized in moderate yield via an o-naphthoquinone catalyzed tandem cross-coupling of substituted aniline and benzylamine under aerobic oxidation conditions.Recommanded Product: 7-Azaindole-5-boronic Acid Pinacol Ester

Referemce:
Indole alkaloid derivatives as building blocks of natural products from聽Bacillus thuringiensis聽and聽Bacillus velezensis聽and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles