2518-12-9Relevant articles and documents
Compound embodiments that release H2S by reaction with a reactive compound and methods of making and using the same
-
, (2021/08/04)
Disclosed herein are embodiments of a donor compound that releases H2S by reacting with a reactive compound. The donor compound embodiments described herein can be used to deliver H2S to a subject or a sample and further can be used to administer therapeutic agents. The donor compound embodiments also can facilitate bioconjugation. Methods of making and using the donor compound embodiments also are disclosed.
Thiazoline-Iridium (III) Complexes and Immobilized Nanomaterials as Selective Catalysts in N-Alkylation of Amines with Alcohols
Denizalt?, Serpil,Dayan, Serkan,Günnaz, Salih,?ahin, Ertan
, (2020/10/02)
In this research, a new series of thiazoline-iridium (III) complexes (4–7) derived from cysteine were prepared and fully characterized by conventional methods. The molecular structure of complex 5 was also determined by single-crystal X-ray diffraction. These complexes were evaluated as catalysts for hydrogen-borrowing reactions of amines with alcohols. In particular, complex 5 showed the best activity as catalyst. Various amines have been alkylated with alcohols affording moderate to good yield (33–99%). Moreover, the immobilized nanomaterials (M1,2) were fabricated by sonication process from the best catalyst 5 with the multi-walled carbon nanotubes (MWCNTs) and graphene oxide (GO), respectively, and characterized by X-ray diffraction (XRD), Fourier transform infrared (FT-IR) spectroscopy, field emission scanning electron microscopy (FE-SEM), energy dispersive X-ray (EDX) spectroscopy, and inductively coupled plasma-mass spectrometry (ICP-MS). The M1,2 nanomaterials were also tested as catalysts in model catalytic reaction for N-alkylation. The M1 nanomaterial showed significantly higher activity than the M2 nanomaterial. The M1 catalyst was recovered by filtration and reused for four catalytic cycles with high conversion (99%, 97%, 96%, and 86%).
Thionoesters: A Native Chemical Ligation-Inspired Approach to Cysteine-Triggered H2S Donors
Cerda, Matthew M.,Zhao, Yu,Pluth, Michael D.
supporting information, p. 12574 - 12579 (2018/10/02)
Native chemical ligation (NCL) is a simple, widely used, and powerful synthetic tool to ligate N-terminal cysteine residues and C-terminal α-thioesters via a thermodynamically stable amide bond. Building on this well-established reactivity, as well as adv
Method for preparing 2,4-disubstituted thiazoline compound from acyl chloride
-
Paragraph 0046; 0047; 0048; 0049; 0050; 0051, (2017/05/23)
The invention provides a novel method for preparing 2,4-disubstituted thiazoline at high yield by firstly reacting acyl chloride serving as a raw material and beta-azide disulfide and also provides a general formula I and application of a product, namely a 2,4-disubstituted thiazoline compound. By using the method, the defects of synthesis complexity, high byproduct yield and slightly low yield of the existing method are overcome, and the method has the advantages of high yield (up to 90% or above), high repeatability and suitability for preparation on a relatively large scale.
One-Pot Strategy for Thiazoline Synthesis from Alkenes and Thioamides
Alom, Nur-E,Wu, Fan,Li, Wei
supporting information, p. 930 - 933 (2017/02/26)
A convenient synthesis of a privileged pharmaceutical motif, thiazoline is accomplished. This reaction utilizes simple and readily available alkene and thioamide substrates in an intermolecular fashion via a simple one-pot procedure. A wide range of functional groups is tolerated, and the thiazoline product has been further utilized for the synthesis of the corresponding β-aminothiol and thiazole from routine hydrolysis and oxidation protocols.
Cu(i)-Catalyzed oxidative homo-coupling of thiazoline-4-carboxylates: Synthesis of 4,4′-bithiazoline derivatives
Fang, Xinxin,Zhang, Kaifan,Yao, Hequan,Huang, Yue
, p. 8030 - 8034 (2016/09/09)
Cu(i)-Catalyzed oxidative homo-coupling of thiazoline-4-carboxylates with good functional group tolerance has been developed. The methodology presented an efficient method to directly construct vicinal carbon-hetero quaternary centers existing in numerous functional molecules and could be applied to the synthesis of 4,4′-bithiazoles which are difficult to prepare by direct C-H activation.
The Synthesis and Biological Evaluation of Anithiactin A/Thiasporine C and Analogues
Lamb, Richard A.,Badart, Michael P.,Swaney, Brooke E.,Gai, Sinan,Baird, Sarah K.,Hawkins, Bill C.
, p. 1829 - 1833 (2015/12/26)
The synthesis of anithiactin A has been achieved in four steps. Several closely related analogues were synthesised and their biological activity against colon and breast cancer cell lines evaluated. Anithiactin A was found not to be cytotoxic even at a hi
Design and synthesis of new 2-aryl-4,5-dihydro-thiazole analogues: In vitro antibacterial activities and preliminary mechanism of action
Tan, Fangfang,Shi, Baojun,Li, Jian,Wu, Wenjun,Zhang, Jiwen
, p. 20118 - 20130 (2015/12/23)
Sixty 2-aryl-4,5-dihydrothiazoles were designed and synthesized in yields ranging from 64% to 89% from cysteine and substituted-benzonitriles via a novel metal- and catalyst-free method. The structures of the title compounds were confirmed mainly by NMR spectral data analysis. Antibacterial activity assays showed that the compounds (S)-2-(2′-hydroxyphenyl)-4-hydroxy-methyl-4,5-dihydrothiazole (7h) and (R)-2-(2′-hydroxyphenyl)-4-hydroxymethyl-4,5-dihydro-thiazole (7h′) exhibited significant inhibition against Ralstonia solanacearum, Pseudomonas syringae pv. actinidiae, Bacillus subtilis and Bacillus cereus, with minimum inhibitory concentrations (MICs) ranging from 3.91 to 31.24 μg·mL-1. The effect of substituents showed that not only electron-withdrawing groups, but also electron-donating groups could abolish the antibacterial activities unless a 2′-hydroxy group was introduced on the 2-aryl substituent of the 4,5-dihydrothiazole analogues. The results of scanning electron microscope (SEM) and fatty acid exposure experiments indicated that these antibacterial compounds influence fatty acid synthesis in the tested bacteria.
Concise synthesis of 2,4-disubstituted thiazoles from β-azido disulfides and carboxylic acids or anhydrides: Asymmetric synthesis of cystothiazole C
Liu, Yi,Sun, Xue,Zhang, Xing,Liu, Jun,Du, Yuguo
, p. 8453 - 8461 (2014/12/10)
A novel and efficient method for the one-pot synthesis of 2,4-disubstituted thiazoles from carboxylic acids or anhydrides is presented. Based on this new method, the total synthesis of the bis-2,4-disubstituted bis(thiazoles) natural product cystothiazole C is also presented. This journal is
Convenient Synthesis of Azolines to Azoles
-
Paragraph 0095, (2013/03/26)
Azolines are oxidized in the presence of a copper-containing catalyst to azoles in the presence of molecular oxygen. A synthetic scheme converting azolines azoles is also provided.
