4667-99-6Relevant articles and documents
Semisynthetic Antimycobacterial C-3 Silicate and C-3/C-21 Ester Derivatives of Fusidic Acid: Pharmacological Evaluation and Stability Studies in Liver Microsomes, Rat Plasma, and Mycobacterium tuberculosis culture
Njoroge, Mathew,Kaur, Gurminder,Espinoza-Moraga, Marlene,Wasuna, Antonina,Dziwornu, Godwin Akpeko,Seldon, Ronnett,Taylor, Dale,Okombo, John,Warner, Digby F.,Chibale, Kelly
, p. 1634 - 1644 (2019)
Fusidic acid (FA), a natural product fusidane triterpene-based antibiotic with unique structural features, is active in vitro against Mycobacterium tuberculosis, the causative agent of tuberculosis (TB). While possessing good pharmacokinetics in man, FA is rapidly metabolized in rodents, thus complicating proof-of-concept studies in this model. Toward the repositioning of FA as an anti-TB agent, we herein describe the synthesis, activity, and metabolism of FA and semisynthesized ester derivatives in rat liver microsomes, rat plasma, and mycobacterial cell culture. FA and derivative molecules with a free C-3 OH underwent species-specific metabolism to the corresponding 3-OH epimer, 3-epifusidic acid (3-epiFA). FA was also metabolized in rat plasma to form FA lactone. These additional routes of metabolism may contribute to the more rapid clearance of FA observed in rodents. C-3 alkyl and aryl esters functioned as classic prodrugs of FA, being hydrolyzed to FA in microsomes, plasma, and Mycobacterium tuberculosis culture. In contrast, C-3 silicate esters and C-21 esters were inert to hydrolysis and so did not act as prodrugs. The antimycobacterial activity of the C-3 silicate esters was comparable to that of FA, and these compounds were stable in microsomes and plasma, identifying them as potential candidates for evaluation in a rodent model of tuberculosis.
Synthesis of triethoxysilanol
Kazakova,Gorbatsevich,Skvortsova,Demchenko,Muzafarov
, p. 1350 - 1351 (2005)
Triethoxysilanol was isolated for the first time by hydrolysis of chloro(triethoxy)silane in an organic solvent in the presence of a heterogeneous base and identified as an individual compound. The synthesis of this compound made it possible to study its physicochemical properties and substantially extended its potentialities for the synthesis of hyperbranched polyethoxysiloxanes and functional oligomers.
Industrial synthesis method of triethoxychlorosilane
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Paragraph 0040-0077, (2021/05/05)
The invention relates to the field of organic synthesis, aims to overcome the defects of high content of byproducts, low selectivity of triethoxychlorosilane and the like in preparation of triethoxychlorosilane by using triethoxysilane as a raw material and adopting a chlorination reaction, and provides a method for converting the triethoxysilane into the triethoxychlorosilane by using trichloroisocyanuric acid as a chlorination reagent and halogenated metal salt as an additive. The method for converting the triethoxysilane into the triethoxychlorosilane has the advantages of high conversion rate of the triethoxysilane, low content of byproducts, high selectivity of the triethoxychlorosilane and small separation load, and is particularly suitable for industrial preparation of the triethoxychlorosilane.