103342-27-4Relevant articles and documents
Discovery and Characterization of XY101, a Potent, Selective, and Orally Bioavailable RORγInverse Agonist for Treatment of Castration-Resistant Prostate Cancer
Zhang, Yan,Wu, Xishan,Xue, Xiaoqian,Li, Chenchang,Wang, Junjian,Wang, Rui,Zhang, Cheng,Wang, Chao,Shi, Yudan,Zou, Lingjiao,Li, Qiu,Huang, Zenghong,Hao, Xiaojuan,Loomes, Kerry,Wu, Donghai,Chen, Hong-Wu,Xu, Jinxin,Xu, Yong
, p. 4716 - 4730 (2019)
We report the design, optimization, and biological evaluation of nuclear receptor RORγinverse agonists as therapeutic agents for prostate cancer treatment. The most potent compound 27 (designated as XY101) exhibited cellular activity with an IC50/su
Synthesis method of O-formate benzyl sulfonamide
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, (2021/10/30)
The invention discloses a synthesis method of ortho-formate benzyl sulfonamide, and relates to the technical field of battery electrolyte additives. The method comprises the following steps: taking 2 - chloromethyl benzoate as a raw material, and performing nucleophilic substitution reaction. The oxidation chlorination reaction, the ammoniation reaction and the tert-butyl protection are obtained, that is, the ortho-formate benzyl sulfonamide. To the invention, a plurality of reaction kettles are used for gradually synthesizing the ortho-formate benzyl sulfonamide, the direct connection relation between each product is isolated, the influence of byproducts generated by the solvent on different reactions is avoided, and the purity of the product is further improved by adopting a method of distilled water washing, ethyl acetate extraction and anhydrous magnesium sulfate drying. The total yield of the synthesis method reaches above 59.96%, and the purity of the ortho-formate benzyl sulfonamide reaches 99.5% or above.
Production method of methyl o-formate benzyl sulfonamide
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Page/Page column 6-9, (2020/09/12)
The invention belongs to the technical field of pesticide intermediates, and particularly relates to a production method of methyl o-formate benzyl sulfonamide. The production method comprises steps:reacting o-methylbenzoic acid with sulfuryl chloride to obtain o-chloromethylbenzoic acid; reacting o-chloromethylbenzoic acid with methanol to obtain o-chloromethyl methyl benzoate; reacting o-chloromethyl methyl benzoate with sodium thiosulfate to obtain methyl o-formate benzyl mercaptan, reacting methyl o-formate benzyl mercaptan with chlorine to obtain methyl o-formate benzyl sulfonyl chloride, and reacting methyl o-formate benzyl sulfonyl chloride with ammonia gas to obtain methyl o-formate benzyl sulfonamide. According to the method, polychlorinated side reactions in the production process are reduced, the yield is increased, the tar yield is reduced, and the problems of low yield and high cost in the production process are solved.
INHIBITORS OF CYTOSOLIC PHOSPHOLIPASE A2
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Page/Page column 41, (2008/06/13)
This invention provides chemical inhibitors of the activity of various phospholipase enzymes, particularly cytosolic phospholipase A2 enzymes (cPLA2), more particularly including inhibitors of cytosolic phospholipase A2 alpha enzymes (cPLAα). In some embodiments, the inhibitors have the Formula I: wherein the constituent variables are as defined herein.
Development of an immunoassay for the residues of the herbicide bensulfuron-methyl.
Lee, Jae Koo,Ahn, Ki Chang,Park, Oee Sook,Ko, Yong Kwan,Kim, Dae-Whang
, p. 1791 - 1803 (2007/10/03)
To develop a competitive indirect enzyme-linked immunosorbent assay based on polyclonal antibodies for the detection of the sulfonylurea herbicide bensulfuron-methyl, seven structurally related haptens were synthesized. Four of them mimicking the target analyte were conjugated to keyhole limpet hemocyanin by the N-hydroxysuccinimide activated ester method to use as immunogens, and all of them were conjugated to bovine serum albumin to use as plate-coating antigens. Polyclonal antibodies raised in rabbits and the coating antigens were screened and selected for the assay in simple homologous and heterologous ELISA formats. Three sensitive heterologous ELISAs were selected and optimized, showing the average IC(50) values of bensulfuron-methyl as low as 0.17, 0.09, and 0.09 ng/mL, the detection ranges of 0.04-0.60, 0.01-0.60, and 0.04-0.25 ng/mL, and the lowest detection limits of 0.03, 0.002, and 0.03 ng/mL, respectively. The cross-reactivities of other sulfonylurea herbicides and metabolites of bensulfuron-methyl to the antibodies were less than 15% in the two assays. Recoveries from the analyte-fortified water samples in assay I were in the range of 81-125% by simple dilution. The correlation between the ELISA and HPLC was 0.999 (n = 15) with a slope of 1.37 in the analysis of groundwater samples fortified with bensulfuron-methyl. The results obtained strongly indicate that the ELISA can be a highly sensitive and convenient tool for detecting bensulfuron-methyl residues in agricultural and environmental samples.
Process for preparing o-(carboalkoxy)phenylmethanesulfonyl chloride derivatives
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, (2016/03/01)
A process for preparing an o-(carboalkoxy)phenylmethanesulfonyl chloride derivative of formula (1), wherein: X is chosen from a hydrogen atom, halogen atoms, C1to C6alkyl groups, C1to C6haloalkyl groups, C1to C6alkoxy groups, C1to C6alkoxycarbonyl groups, a nitro group, and a phenyl group; R is chosen from C1to C6alkyl groups, C1to C6haloalkyl groups, and C3to C6cycloalkyl groups; and n is chosen from integers ranging from 1 to 4, is discussed.
Alkoxide-catalyzed ring-opening of a novel homosaccharin derivative: Synthesis of potent, selective P3-lactam thrombin inhibitors containing P4- o-alkoxycarbonylbenzylsulfonamide residues
Owens, Timothy D.,Semple, J. Edward
, p. 3683 - 3688 (2007/10/03)
A series of lactam derivatives 1b-g featuring P4-o- alkoxycarbonylbenzylsulfonamide residues along with the potential P4- homosaccharin prodrug candidate 1h was prepared in order to probe the thrombin S3 specificity pocket. The synthesis and alkoxide-catalyzed ring opening of the novel homosaccharin intermediate 7 followed by subsequent elaboration delivered the targets 1b-h which were potent and selective thrombin inhibitors. The design, synthesis, and biological activity of these targets will be presented.
Herbicidal compounds, their production and use
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, (2008/06/13)
A compound of the general formula STR1 wherein R1 is a phenyl group which may be substituted, R2 and R3 respectively are a lower alkyl or lower alkoxy group, Z is CH or N and n is 0 or 1, or a salt thereof which is useful as a herbicide.