52133-67-2Relevant articles and documents
PROCESS AND INTERMEDIATES FOR PREPARING A JAK INHIBITOR
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, (2022/03/04)
The present invention is related to processes for preparing ruxolitinib, or a salt thereof, and related synthetic intermediates related thereto.
PROCESS AND INTERMEDIATES FOR PREPARING A JAK1 INHIBITOR
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, (2022/03/02)
The present invention is related to processes for preparing itacitinib, or a salt thereof, and related synthetic intermediates related thereto.
Synthesis and biological evaluation of some new tricyclic pyrrolo[3,2-e]tetrazolo[1,5-c]pyrimidine derivatives as potential antitubercular agents
Patil, Yogesh,Shingare, Ramesh,Choudhari, Amit,Borkute, Rachana,Sarkar, Dhiman,Madje, Balaji R.
, (2018/08/07)
A series of new tricyclic pyrrolo[3,2-e]tetrazolo[1,5-c]pyrimidines 8a–l were synthesized and characterized by IR, NMR (1H and 13C), and mass spectral analysis. The newly synthesized compounds 8a–l were inspected for their in vitro antitubercular activity against Mycobacterium tuberculosis (MTB) H37Ra using an established XTT reduction menadione assay (XRMA). The title compounds exhibited minimum inhibitory concentrations (MIC90) ranging from 0.09 to >30 μg/mL. Five compounds (8c, 8i–l) were further confirmed for their dose-dependent effect against MTB. These compounds were evaluated in the THP-1 infection model, where 8i (MIC90 = 0.35 μg/mL), 8j (MIC90 = 1.17 μg/mL), 8k (MIC90 = 2.38 μg/mL), and 8l (MIC90 = 1.17 μg/mL) demonstrated significant antitubercular activity. All the ex vivo active compounds showed insignificant cytotoxicity against the human cancer cell lines, HeLa, MCF-7, and THP-1. Inactivity of all these compounds against Gram positive and Gram negative bacteria indicates their specificity. Molecular docking studies in the active site of the sterol 14alpha-demethylase (CYP51) enzyme revealed a similar binding mode to the native ligand in the crystal structure, thereby helping to understand the ligand–protein interactions and to establish a structural basis for inhibition of MTB. The results suggest novel pharmacophores as selective and specific inhibitors against MTB that can be explored further to synthesize lead compounds against tuberculosis. In summary, the results clearly indicate the identification of some novel, selective, and specific inhibitors against MTB that can be explored further for potential antitubercular drugs.
Synthetic method of 4-chloropyrrolopyrimidine
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Paragraph 0008; 0017, (2018/12/05)
The invention relates to a synthetic method of 4-chloropyrrolopyrimidine. The synthetic method takes ethyl cyanoacetate, bromoacetaldehyde diethyl acetal, thiourea, sodium ethoxide and hydrogen peroxide as raw materials and takes DMF, ethanol, water and phosphorous oxychloride as solvents to obtain the target product 4-chloropyrrolopyrimidine through four steps of reactions. The method improves amethod of removing a mercapto group in a third step. The mercapto group is first oxidized to sulfinic acid by using the hydrogen peroxide and then is removed under acidic conditions. The method is mild in reaction conditions, safe in operation and high in yield, is environmentally friendly, and is suitable for industrial production.
The therapeutic compound, use and related method (by machine translation)
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Paragraph 1270; 1271, (2017/06/29)
PROBLEM TO BE SOLVED: To provide a pharmaceutical composition containing a compound or its salt which prevents or treats a central nervous system disease in which integration dysfunction syndrome and agnosia are enumerated as exemplary disorders.SOLUTION: The pharmaceutical composition includes the compound or its salt represented by chemical formula (A) which modulates striatal-enriched protein tyrosine phosphatase (STEP).
One-Pot Synthesis of 3-Substituted 2-Arylpyrrole in Aqueous Media via Addition-Annulation of Arylboronic Acid and Substituted Aliphatic Nitriles
Yousuf, Md,Adhikari, Susanta
supporting information, p. 2214 - 2217 (2017/05/12)
Pd(II)-catalyzed C-C coupling reactions between substituted aliphatic nitriles and arylboronic acids followed by in situ cyclodehydration have been employed for the first time to synthesize a wide variety of 3-substituted 2-aryl-1H-pyrroles in aqueous acetic acid. This one-pot synthesis is green, and it conforms to atom economy. The structures of two representative pyrroles, 3k and 5f, were confirmed by X-ray crystallographic analysis.
6-methyl 7-position-denitrified purine nucleoside compounds and application thereof
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Paragraph 0091; 0093; 0094; 0095, (2017/09/02)
The invention discloses6-methyl 7-position-denitrified purine nucleoside compounds and an application thereof and belongs to the field of medicinal chemistry. The 6-methyl 7-position-denitrified purine nucleoside compounds or pharmaceutically acceptable salts of the compounds having characteristics of a structure shown as formula I are a kind of novel-structured compounds designed and synthesized according to protein structure characteristics of RNA virus polymerase, and the compounds can inhibit RNA viruses, thereby being capable of serving as potential drugs for preventing and treating infection of RNA viruses such as HCV (hepatitis c virus), influenza virus, HRV (rhinovirus), RSV, Ebola virus, DENV (Dengue virus), enterovirus and the like.
Alkylation of methylene-active compounds with halo acetals and hydrolysis of the alkylation products
Ismailov,Yusubov,Sadykhova,Gasymov,Ibragimova,Mamedov
, p. 1390 - 1393 (2016/11/29)
A preparative procedure has been proposed for the alkylation of CH acids with halo acetals and hydrolysis of the alkylation products to furan derivatives and lactones.
PYRIMIDINE COMPOUNDS AND PYRIMIDO INDOLE COMPOUNDS AND METHODS OF USE
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Page/Page column 50, (2016/03/19)
The present invention discloses substituted pyrimidine and pyrimido indole compounds and optionally pharmaceutically acceptable salts, hydrates or solvates thereof. A method of treating a patient having cancer or a disease comprising administering to a patient an effective amount of the compound or pharmaceutically acceptable salt, hydrate, or solvate thereof.
THERAPEUTIC COMPOUNDS AND RELATED METHODS OF USE
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Paragraph 1563, (2015/11/16)
Methods of treating disorders using compounds that modulate striatal-enriched tyrosine phosphatase (STEP) are described herein. Exemplary disorders include schizophrenia and cognitive deficit.