3131-63-3Relevant articles and documents
Efficient cyclization of 2-phenoxyalkanals to 2-alkylbenzo[b]furans
Witczak,Kwiecien
, p. 2223 - 2230 (2005)
A new and efficient route to 2-alkylbenzo[b]furans via acid-catalyzed cyclization of 2-phenoxyalkanals under mild conditions over amberlyst-15 resin has been described. Copyright Taylor & Francis, Inc.
NOVEL COMPOUND AND PHARMACEUTICAL COMPOSITION COMPRISING SAME FOR ENHANCING ANTICANCER ACTIVITY
-
Paragraph 0104-0105, (2021/11/04)
The present invention relates to a novel compound and a pharmaceutical composition for enhancing anticancer activity, which includes the same, and more particularly, to a pharmaceutical composition, which includes a compound represented by Formula 1 or a pharmaceutically acceptable salt thereof, thereby enhancing anticancer activity of an anticancer agent or radiation, and inducing proliferation inhibition and death of cancer cells, resulting in effectively treating cancer: In Formula 1, n is an integer of 0 to 4; R1 is hydrogen, C1 to C10 alkyl or aryl(C1 to C4)alkyl; R3 is C1 to C6 alkyl, and when there are a plurality of the R3, the R3s are the same or different; L1 is a direct bond, or C1 to C6 alkylene; R2 is hydrogen, C1 to C10 alkyl or aryl(C1 to C4)alkyl, and R4 is hydrogen, C1 to C4 alkyl, C3 to C8 cycloalkyl or aryl(C1 to C4)alkyl, or R2 and R4 are connected to form a 4 to 7-membered ring; and the alkyl of R1 to R4, the arylalkyl of R1, R2 and R4, the cycloalkyl of R4, the alkylene of L1 are each independently unsubstituted or substituted with a substituent such as a C1 to C6 alkyl group, a halo group, an aryl group, a haloalkyl group, a nitro group, a cyano group, an alkylthio group or an arylalkylthio group, and when the compound is substituted with a plurality of substituents, the substituents are the same or different.
Preparation method of benzofuran compound
-
Paragraph 0114-0117, (2019/04/04)
The invention relates to a preparation method of a benzofuran compound. The preparation method comprises the following steps: putting a furan compound, acetic acid and a Lewis acid catalyst in a reaction vessel, reacting for 0.5-24 h at 80-160 DEG C, and separating and purifying to obtain the benzofuran compound. According to the preparation method provided by the invention, the furan compound isused as a reaction raw material, an acetic acid water solution is used as a solvent, Lewis acid is used as a catalyst, and at a mild reaction temperature (80-160 DEG C), the benzofuran compound is directly obtained through one-step reaction. The preparation method provided by the invention can synthesize the benzofuran compound with a corresponding structure and functional groups based on the structure and functional groups of the furan compound as a raw material, the raw material components are simple , and the process is convenient to operate; wherein the selectivity of the obtained benzofuran is as high as 99% in the process of synthesizing benzofuran by using furan, so that the method has industrial application prospects.
Glutathione conjugation and protein adduction derived from oxidative debromination of benzbromarone in mice
Wang, Hui,Wang, Wenbao,Gong, Bowen,Wang, Zedan,Feng, Yukun,Zhang, Weige,Wang, Shaojie,Peng, Ying,Zheng, Jiang
, p. 1281 - 1290 (2019/11/20)
Benzbromarone (BBR), a uricosuric agent, has been known to induce hepatotoxicity, and its toxicity has a close relation to cytochrome P450-mediated metabolic activation. An oxidative debromination metabolite of BBR has been reported in microsomal incubations. The present study attempted to define the oxidative debromination pathway of BBR in vivo. One urinary mercapturic acid (M1) and one glutathione (GSH) conjugate (M2) derived from the oxidative debromination metabolitewere detected in BBR-treated mice after solid phase extraction.M1 andM2 shared the same chromatographic behavior and mass spectral identities as those detected in N-acetylcysteine/GSHand BBR-fortified microsomal incubations. The structure of M1 was characterized by chemical synthesis, along with mass spectrometry analysis. In addition, hepatic protein modification that occurs at cysteine residues (M93) was observed in mice given BBR. The observed protein adduction reached its peak 4 hours after administration and occurred in a dose-dependent manner. A GSH conjugate derived from oxidative debromination of BBR was detected in livers of mice treated with BBR, and the formation of the GSH conjugate apparently took place earlier than the protein adduction. In summary, our in vivo work provided strong evidence for the proposed oxidative debromination pathway of BBR, which facilitates the understanding of the mechanismsof BBR-induced hepatotoxicity. SIGNIFICANCE STATEMENT This study investigated the oxidative debromination pathway of benzbromarone (BBR) in vivo. One urinary mercapturic acid (M1) and one glutathione (GSH) conjugate (M2) derived from the oxidative debromination metabolite were detected in BBR-treated mice. M1 and M2 were also observed in microsomal incubations. The structure of M1 was characterized by chemical synthesis followed by mass spectrometry analyses. More importantly, protein adduction derived fromoxidative debromination ofBBR(M93) was observed in mice given BBR, and occurred in dose- and time-dependent manners. The success in detection of GSH conjugate, urinary N-acetylcysteine conjugate, and hepatic protein adduction in mice given BBR provided solid evidence for in vivo oxidative debromination of BBR. The studies allowed a better understanding of the metabolic activation of BBR.