13831-31-7Relevant articles and documents
Rosuvastatin calcium intermediate, preparation method thereof and application of intermediate
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Paragraph 0055; 0056; 0058, (2019/04/17)
The invention discloses a rosuvastatin calcium intermediate, a preparation method thereof and an application of the intermediate. The synthesis process of the intermediate is environmentally friendly,simple and convenient to operate and low in EHS (environment health safety) risk, raw materials are easily available, and used chemical reagents are low in toxicity and low in price, so that the synthesis process of the intermediate is a green synthesis process suitable for industrial production. In addition, the intermediate is applied to synthesis of rosuvastatin calcium and key intermediates thereof, has short route and high yield, effectively reduces the industrial production cost of rosuvastatin calcium, and has a higher industrial application prospect.
Synthesis and evaluation of novel monosubstituted sulfonylurea derivatives as antituberculosis agents
Pan, Li,Jiang, Ying,Liu, Zhen,Liu, Xing-Hai,Liu, Zhuo,Wang, Gang,Li, Zheng-Ming,Wang, Di
scheme or table, p. 18 - 26 (2012/07/01)
A series of novel monosubstituted sulfonylurea derivatives 10a-y were synthesized and characterized by 1H NMR, 13C NMR and HRMS. These compounds were evaluated against Mycobacterium tuberculosis H37Rv in vitro. The results showed compounds 10f, 10k and 10s exhibited moderate antituberculosis activities with MIC values in the range of 20-100 mg/L. Compounds 10b and 10o displayed good antituberculosis activities (MIC 10 mg/L), which were comparable with that of the sulfometuron methyl. Both of the two compounds showed little cytotoxicities, with an IC50 against THP-1 cells greater than 100 mg/L.
4,4-Bis(methylthio)azetidin-2-ones as synthons of 1,2- and 1,3-dicarbonyl systems
Konaklieva, Monika I.,Suwandi, Lita S.,Kostova, Maya,Deschamps, Jeffrey
supporting information; experimental part, p. 1909 - 1912 (2011/04/25)
The importance of β-lactams as synthetic building blocks has been widely recognized in organic synthesis due to possible ring cleavage at any of the four single bonds of the β-lactam ring. We now report reactions involving breaking of the N1-C4 bond in differently substituted at C3 4,4-bis(methylthio)azetidin-2-ones, leading to formation of 1,2- and 1,3-dicarbonyl systems.
P38 MAP KINASE INHIBITORS
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Page/Page column 42-43, (2010/07/02)
The present disclosure relates to compounds of formula (I): which are inhibitors of p38 mitogen-activated protein kinase enzymes,particularly the alpha and gamma kinase sub-types thereof, and their use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, such as COPD
SUBSTITUTED CYCLOHEXYL-1,4-DIAMINE DERIVATIVES WITH A CHAIN EXTENSION
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Page/Page column 25, (2008/06/13)
The invention relates to substituted cyclohexyl-1,4-diamine derivatives, to a method for their production, to medicaments containing said compounds and to the use of substituted cyclohexyl-1,4-diamine derivatives for producing medicaments.
Synthesis of 3-acetoxyazetidin-2-ones and 3-hydroxyazetidin-2-ones with antifungal and antibacterial activity
Walsh,Meegan,Prendergast,Al Nakib
, p. 989 - 1000 (2007/10/03)
The synthesis of a series of 3-acetoxyazetidin-2-ones 3a-n and 3-hydroxyazetidin-2-ones 6a-j is reported together with the antibacterial and antifungal evaluation of these compounds. An additional series of 3-acetoxyazetidin-2-ones 11a-h which possess a free carboxylic acid group on the N-1 aryl ring were obtained by treatment of suitably substituted Schiff bases 10a-h with acetoxyacetyl chloride. The novel bicyclic structures 7-acetoxy-6-phenyl-5-thia-1-azabicyclo[4.2.0]octan-8-one 13 and 7-hydroxy-6-phenyl-5-thia-1-azabicyclo[4.2.0]octan-8-one 14 were also obtained. Many of the compounds displayed antifungal activity in vitro when evaluated against the pathogenic fungi Cryptococcus neoformans, Candida albicans, Candida tropicalis, Candida parapsilosis, Candida glabrata, and Trichosporon cutaneum, while 3-acetoxyazetidin-2-ones 11a-h containing a free carboxylic acid group on the N-1 aryl ring displayed antibacterial activity against Staphylococcus aureus, Proteus vulgaris, Pseudomonas aeruginosa, Bacillus subtilis, Klebsiella aerogenes and Escherischia coli.
A New Chemoenzymatic Approach to the Synthesis of Penems
Altamura, Maria,Cesti, Pietro,Francalanci, Franco,Marchi, Marcello,Cambiaghi, Stefano
, p. 1225 - 1229 (2007/10/02)
A new synthesis of the valuable penem antibiotics FCE 22101 and FCE 22891 which does not require the use of expensive protecting groups is reported.A mixed carbon-silicon protection of two hydroxy groups was used, followed by a selective enzymatic hydrolysis of the resulting 8-O-protected-2-carboxylic ester (18).Lipase from Chromobacterium viscosum and lipoprotein lipase from Pseudomonas sp. gave excellent results in both free or immobilized form.
Benzothiazole substituted carboxylic acid amide compounds and herbicidal methods compositions thereof
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, (2008/06/13)
Novel substituted carboxylic acid amide compound of the formula STR1 wherein n is an integer from 1 to 4 each R is independently selected from hydrogen, halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio, haloalkylthio, amino, alkylamino, dialkylamino, nitro, cyano and alkoxycarbonyl; and two R radicals taken together can represent methylenedioxy, dichloromethylenedioxy or difluoromethylenedioxy, R1 is hydrogen or alkyl, R2 and R3 are individually selected from hydrogen or a radical selected from alkyl, alkenyl, alkynyl, aralkyl, cycloalkyl, aryl and nitrogen-containing heterocycles, each of which radicals may be substituted and each of which radicals may, together with the nitrogen atom to which they are attached, form an optionally substituted, optionally partially unsaturated and optionally benzofused monocyclic or bicyclic radical, which may contain one or more further hetero-atoms, and X is oxygen or sulfur.
New Antihypertensive Cannabinoids
Zaugg, Harold E.,Kyncl, Jaroslav
, p. 214 - 217 (2007/10/02)
A number of azacannabinoids containing hydroxyacyl and aminoacetyl substituents on the nitrogen atom were synthesized.The hydroxyacetyl and γ-hydroxybutyryl derivatives (4a and 7b, respectively) were potent antihypertensive agents (minimum effective dose, 3-5 mg/kg, orally) of the same order of activity as the highly CNS-active N-propargyl derivatives Ia and Ib.Furthermore, 4a showed weak stimulant properties at hypotensive dose levels, in contrast to the strongly CNS-depressant action characteristic of the N-propargyl analogues (Ia,b).
Triiodoisophthalamide X-ray contrast agent
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, (2008/06/13)
Novel X-ray contrast agents, i.e., N,N'-bis(2,3-dihydroxypropyl)-5-N-(2-hydroxyethyl)glycolamido-2,4,6-triiodoisophthalamide.
