28819-05-8Relevant articles and documents
Sparsomycin analogs. II. Synthesis and biological activities of 5-carboxy-6-methyluracil derivatives
Kanamoto,Nagai,Hase,et al.
, p. 135 - 143 (1983)
In order to study the structure-activity relationship of sparsomycin, an antitumor antibiotic, 26 sparsomycin-related compounds were synthesized and their antibacterial activities and lytic actions on Ehrlich ascites carcinoma cells were tested.
Enantioconvergent Cu-Catalyzed Radical C-N Coupling of Racemic Secondary Alkyl Halides to Access α-Chiral Primary Amines
Cheng, Jiang-Tao,Dong, Xiao-Yang,Gu, Qiang-Shuai,Li, Zhong-Liang,Liu, Juan,Liu, Xin-Yuan,Luan, Cheng,Wang, Fu-Li,Wang, Li-Lei,Yang, Ning-Yuan,Zhang, Yu-Feng
, p. 15413 - 15419 (2021/09/30)
α-Chiral alkyl primary amines are virtually universal synthetic precursors for all other α-chiral N-containing compounds ubiquitous in biological, pharmaceutical, and material sciences. The enantioselective amination of common alkyl halides with ammonia is appealing for potential rapid access to α-chiral primary amines, but has hitherto remained rare due to the multifaceted difficulties in using ammonia and the underdeveloped C(sp3)-N coupling. Here we demonstrate sulfoximines as excellent ammonia surrogates for enantioconvergent radical C-N coupling with diverse racemic secondary alkyl halides (>60 examples) by copper catalysis under mild thermal conditions. The reaction efficiently provides highly enantioenrichedN-alkyl sulfoximines (up to 99% yield and >99% ee) featuring secondary benzyl, propargyl, α-carbonyl alkyl, and α-cyano alkyl stereocenters. In addition, we have converted the masked α-chiral primary amines thus obtained to various synthetic building blocks, ligands, and drugs possessing α-chiral N-functionalities, such as carbamate, carboxylamide, secondary and tertiary amine, and oxazoline, with commonly seen α-substitution patterns. These results shine light on the potential of enantioconvergent radical cross-coupling as a general chiral carbon-heteroatom formation strategy.
Substituted macrocyclic tyrosine kinase inhibitor and application thereof
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Paragraph 0206-0210, (2021/07/21)
The invention belongs to the technical field of medicines, and particularly relates to a substituted macrocyclic tyrosine kinase inhibitor compound, and pharmaceutically acceptable salts and stereoisomers thereof. More specifically, the tyrosine kinase is
Preparation method of carboxylic ester compound
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Paragraph 0044-0045, (2021/03/30)
The invention relates to a preparation method of a carboxylic ester compound, which comprises the following steps: reacting carboxylic acid with methanol in air under the catalysis of nitrite to obtain an ester compound, the preparation method disclosed by the invention has the advantages of rich raw material sources, cheap and easily available catalyst, mild reaction conditions, simplicity and convenience in operation and the like, a series of fatty carboxylic acids can be modified with high yield, and particularly, the traditional esterification method is generally not suitable for esterification of drug molecules. By utilizing the method, a series of known drug molecules can be modified, so that a shortcut is provided for discovering new drug molecules.
Green Esterification of Carboxylic Acids Promoted by tert-Butyl Nitrite
Cheng, Xionglve,Jiang, Gangzhong,Li, Xingxing,Tao, Suyan,Wan, Xiaobing,Zhao, Yanwei,Zheng, Yonggao
supporting information, p. 2713 - 2718 (2021/06/25)
In this work, the green esterification of carboxylic acids promoted by tert-butyl nitrite has been well developed. This transformation is compatible with a broad range of substrates and exhibits excellent functional group tolerance. Various drugs and substituted amino acids are applicable to this reaction under near neutral conditions, with good to excellent yields.
A Mild, General, Metal-Free Method for Desulfurization of Thiols and Disulfides Induced by Visible-Light
Qiu, Wenting,Shi, Shuai,Li, Ruining,Lin, Xianfeng,Rao, Liangming,Sun, Zhankui
supporting information, p. 1255 - 1258 (2021/05/05)
A visible-light-induced metal-free desulfurization method for thiols and disulfides has been explored. This radical desulfurization features mild conditions, robustness, and excellent functionality compatibility. It was successfully applied not only to the desulfurization of small molecules, but also to peptides.
C-terminal 1-aminoethyltetrazole-containing oligopeptides as novel alanine racemase inhibitors
Anderson, Rosaleen J.,Gray, Mark,Kondacs, Laszlo A.,Marrs, Emma C. L.,Orenga, Sylvain,Perry, John D.
, (2020/03/19)
In clinical culture media inoculated with patient samples, selective inhibition of commensal bacteria is essential for accurate diagnosis and effective treatment, as they can mask the presence of pathogenic bacteria. The alanine analogue, 1-aminoethyltetr
ANTIBACTERIAL COMPOUND AND USES OF SAME
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Paragraph 0048-0049, (2020/09/15)
A new compound exhibiting particularly advantageous antibacterial properties, and having the structural formula: L-pyroglutamyl-L-1-aminoethyltetrazole (or N-(1-(1H-tetrazol-5-yl)ethyl)-5-oxopyrrolidine-2-carboxamide). Also, the use of this compound in mi
Desulfurization method of organic compounds containing mercapto or disulfide bond
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Paragraph 0026, (2019/10/01)
The invention relates to a desulfurization method of organic compounds, in particular, organic compounds containing mercapto or a disulfide bond. The method comprises following steps: dissolving organic compounds containing mercapto or a disulfide bond by a solvent; adding a phosphine reagent and an initiator; and carrying out reactions in the presence of light to convert the substrate into corresponding desulfurization products. The organic compounds containing mercapto or a disulfide bond is R-SH or R-S-S-R; wherein R represents a primary carbon group, a secondary carbon group, a tertiary carbon group, an aryl group, or an acyl group. The reactions do not need any metal, and the reaction conditions are mild. Moreover, the desulfurization method has the advantages of high yield, wide substrate application range, and multiple suitable solvents, and is widely suitable for multiple kinds of mercapto-removing reactions and desulfurization reactions of disulfide.
Method for selective removal of t-butyloxycarboryl from nitrogen
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Paragraph 0024-0025; 0026-0028; 0044-0046, (2018/03/26)
The invention discloses a method for selective removal of t-butyloxycarboryl from nitrogen. According to the synthesis method, directed at a reaction substrate having t-butyloxycarboryl and another acyl protecting group on a molecular nitrogen atom, in the presence of a selectfluor reagent, reaction is carried out in a solution for selective removal of t-butyloxycarboryl and retention of another acyl protecting group. The synthesis method provided by the invention is novel and efficient, is not reported in literature, and can be widely used in total synthesis and drug intermediate synthesis.