56926-34-2

Upstream product

• 19082-52-1 4-phenoxyphenyl acetate 
• 56926-42-2 2-hydroxy-5-phenoxy-benzoic acid 
• 917-54-4 methyllithium 
• 56926-45-5 Ethyl-2-benzyloxy-5-phenoxybenzoat 
• 56926-47-7 2-Benzyloxy-5-phenoxybenzoesaeure 
• 56926-43-3 Ethyl-5-phenoxysalicylat 
• 56926-49-9 2-Benzyloxy-5-phenoxy-acetophenon 

Downstream Products

• 84942-38-1 1-(2-Hydroxy-3-nitro-5-phenoxy-phenyl)-ethanone 
• 56926-36-4 Ethyl-2,4-dioxo-4-(2'-hydroxy-5'-phenoxyphenyl)-butyrat 
• 84942-34-7 2-Amino-6-ethyl-4-phenoxy-phenol; hydrochloride 

Relevant academic research and scientific papers

Preparation method of Roxadustat intermediate

The invention discloses a preparation method of a Roxadustat intermediate (A). The method is characterized in that synthesis routes are defined in the description. The method is simple in process, economical and environmentally friendly, thionyl chloride

Activity of Fluorine-Containing Analogues of WC-9 and Structurally Related Analogues against Two Intracellular Parasites: Trypanosoma cruzi and Toxoplasma gondii

Two obligate intracellular parasites, Trypanosoma cruzi, the agent of Chagas disease, and Toxoplasma gondii, an agent of toxoplasmosis, upregulate the mevalonate pathway of their host cells upon infection, which suggests that this host pathway could be a potential drug target. In this work, a number of compounds structurally related to WC-9 (4-phenoxyphenoxyethyl thiocyanate), a known squalene synthase inhibitor, were designed, synthesized, and evaluated for their effect on T. cruzi and T. gondii growth in tissue culture cells. Two fluorine-containing derivatives, the 3-(3-fluorophenoxy)- and 3-(4-fluorophenoxy)phenoxyethyl thiocyanates, exhibited half-maximal effective concentration (EC50) values of 1.6 and 4.9 μm, respectively, against tachyzoites of T. gondii, whereas they showed similar potency to WC-9 against intracellular T. cruzi (EC50values of 5.4 and 5.7 μm, respectively). In addition, 2-[3- (phenoxy)phenoxyethylthio]ethyl-1,1-bisphosphonate, which is a hybrid inhibitor containing 3-phenoxyphenoxy and bisphosphonate groups, has activity against T. gondii proliferation at sub-micromolar levels (EC50=0.7 μm), which suggests a combined inhibitory effect of the two functional groups.

CERTAIN BENZODIOXOLE, BENZODIOXANE AND BENZODIOXEPIN DERIVATIVES USEFUL AS 5-LIPOXYGENASE INHIBITORS

The invention relates to the compounds of the formula wherein each R independently represents hydrogen, lower alkyl, halogen, trifluoromethyl, lower alkoxy, carbocyclic or heterocyclic aryl, carbocyclic or hetero-cyclic aryloxy, carbocyclic or heterocyclic aryl-lower alkyloxy, carbocyclic or heterocyclic aryl-lower alkyl, C3-C7-cycloalkyl-lower alkyloxy, or Cs-Cv-cycloalk-yloxy; n represents 1, 2, 3 or 4; m represents 0, 1 or 2; A represents a direct bond or lower alkylene; X represents oxygen or sulfur; Ri represents hydrogen, acyl, lower alkoxycarbonyl, aminocarbonyl, mono- or di-lower alkylaminocarbonyl, lower alkenylaminocarbonyl, lower alkynylaminocarbonyl, carbocyclic or heterocy-clic aryl-lower alkylaminocarbonyl, carbocyclic or heterocyclic arylaminocarbonyl, C3-C7-cycloalk-ylaminocarbonyl or C3-C7-cycloalkyl-lower al-kylaminocarbonyl; R2 represents lower alkyl, lower alkoxycarbonyl-lower alkyl, C3-C7-cycloalkyl, carbo-cyclic or heterocyclic aryl, carbocyclic or heterocyclic aryl-lower alkyl, C3-C7-cycloalkyl-lower alkyl, amino, mono- or di-lower alkylamino, lower alkenylamino, lower alkynylamino, carbocyclic or heterocyclic aryl-lower alkylamino, carbocyclic or heterocyclic arylamino, C3-C7-cycloalkylamino, C3-C7-cycloalkyl-lower alkylamino, lower alkoxycarbonyl-lower alkyl-amino or lower alkoxy; R3 and R4 independently repre-sent hydrogen or lower alkyl; and pharmaceuticallyacceptable salts thereof; which are useful as 5-lipoxyge-nase inhibitors.

Synthesis of ethyl 6-substituted-chroman- and -chromone-2-carboxylates. A comparative structure-activity study employing the 6-phenyl and phenoxy analogs in the triton hyperlipidemic rat model.

To explore the effect of lipophilicity on antilipidemic activity in the Triton WR-1339 induced hyperlipidemic rat model we synthesized the 6-cyclohexyl, phenyl, and phenoxy analogs of ethyl chroman-2-carboxylate. Results obtained were analyzed in light of the biological activity observed for the 6-chloro-substituted and unsubstituted chromans, the 6-chlorochroman-4-one ester, and the 6-chloro-, phenyl-, and phenoxychromone esters. The suggestion is made that chromones likely exert their antilipidemic effects by a somewhat different set of mechanisms than do the chromans and clofibrate. Whereas the 6-chlorochromanone ester is inactive, the 6-chlorochromone ester is active in both normal and hyperlipidemic Sprague-Dawley rats. The major differential effect was observed for ethyl 6-cyclohexylchroman-2-carboxylate which did not lower cholesterol levels but returned triglyceride levels to normal in hyperlipidemic rats.