- Debenzylative Sulfonylation of Tertiary Benzylamines Promoted by Visible Light
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An efficient, general, inexpensive, and environmentally friendly photosynthesis of sulfonamides via visible light promoted debenzylative sulfonylation of tertiary benzylamines is described. Compared to the traditional S?N coupling reactions, which are promoted by oxidative C?N bond cleavage of symmetrical tertiary alkylamines, this strategy provides a selective C?N bond cleavage protocol and avoids the use of transition-metal, explosive oxidants, and ligands.
- Fu, Ying,Wu, Qing-Kui,Du, Zhengyin
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supporting information
p. 1896 - 1900
(2021/04/06)
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- Controlled synthesis of N, N-dimethylarylsulfonamide derivatives as nematicidal agents
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Gramine can be intelligently and efficiently supplied with N, N-dimethylamino group and then reacted with the corresponding sulfonyl chlorides to synthesize N, N-dimethylarylsulfonamides. We herein designed and controlled synthesis of N, N-dimethylarylsulfonamide derivatives, and first reported the results of the nematicidal activity of 15 title compounds 3a-o against Meloidogyne incongnita in vitro, respectively. Among all of the title derivatives, compounds 3a, 3c, 3k, and 3o exhibited potent nematicidal activity with median lethal concentration (LC50) values ranging from 0.22 to 0.26 mg/L. Most noteworthy, N, N-dimethyl-4-methoxyphenylsulfonamide (3c) and N, N-dimethyl-8-quinolinesulfonamide (3o) showed the best promising and pronounced nematicidal activity, with LC50 values of 0.2381 and 0.2259 mg/L, respectively.
- Chen, Gen-Qiang,Xia, Yan-Fei,Yang, Jin-Ming,Che, Zhi-Ping,Sun, Di,Li, Shen,Tian, Yue-E,Liu, Sheng-Ming,Jiang, Jia,Lin, Xiao-Min
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p. 1197 - 1206
(2019/12/03)
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- Preparation method of N,N-dimethylsulfamide derivatives
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The invention discloses a preparation method of N,N-dimethylsulfamide derivatives and belongs to the technical field of synthesis of medical compounds. The preparation method comprises the following steps: reacting gramine, a reactant with sulfonyl chloride groups and an alkaline substance with any one of solvents such as CH2Cl2, CH3COCH3 and CH3CN at a temperature of minus 15 DEG C to 80 DEG C for 24-48 hours so as to obtain the product, wherein the molar ratio of the gramine to the reactant to the alkaline substance is (1.0-2.0):(1.2-4.0):(1.5-6.0). The N,N-dimethylsulfamide derivatives can be simply and efficiently prepared withlow cost, and the yield is up to 70-98%.
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Paragraph 0091-0095; 0169
(2019/10/01)
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- Charge-Transfer Complex Promoted Regiospecific C?N Bond Cleavage of Vicinal Tertiary Diamines
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A catalyst-free, charge-transfer complex promoted coupling of sulfonyl chlorides with vicinal tertiary diamines to generate sulfonamides is presented. Mechanistic studies showed that these reactions are proceeded via charge transfer of vicinal tertiary diamines to sulfonyl chlorides, forming the unstable sulfonyl quaternary ammonium like complexes which induced the regiospecific intramolecular C?N bond cleavage of vicinal tertiary diamines. (Figure presented.).
- Fu, Ying,Xu, Qin-Shan,Shi, Chun-Zhao,Du, Zhengyin,Xiao, Caiqin
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supporting information
p. 3502 - 3506
(2018/09/14)
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- Potassium tert-butoxide-mediated metal-free synthesis of sulfonamides from sodium sulfinates and N,N-disubstituted formamides
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By using formamides as amine sources, a novel and efficient KO-t-Bu mediated amination of sodium sulfinates has been developed. The reaction utilizes readily available starting materials under metal-free conditions, thus providing an alternative and attractive route to sulfonamides.
- Bao, Xiaodong,Rong, Xiaona,Liu, Zhiguo,Gu, Yugui,Liang, Guang,Xia, Qinqin
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supporting information
p. 2853 - 2858
(2018/06/25)
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- METHYLAMINE DERIVATIVES AS LYSYSL OXIDASE INHIBITORS FOR THE TREATMENT OF CANCER
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Provided are compounds of the Formula (I), or a pharmaceutically acceptable salt thereof, wherein W, X, Y, Z, x, R1, R2, R3, x and n are defined in the specification. The compounds are inhibitors of lysyl oxidase (LOX) and lysyl oxidase-like (LOXL) family members (LOXL1, LOXL2, LOXL3, LOXL4) and are useful in therapy, particularly in the treatment of cancer. Also disclosed are LOX inhibitors for use in the treatment of a cancer associated with EGFR and biomarkers that predict responsiveness to a LOX inhibitor.
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Paragraph 00728
(2017/09/08)
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- Copper-mediated S-N formation via an oxygen-activated radical process: A new synthesis method for sulfonamides
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Copper-mediated direct S-N formation using readily available starting materials via an oxygen-activated radical process has been developed. This method provides a novel and direct approach for synthesis of sulfonamides under air conditions. the Partner Organisations 2014.
- Huang, Xin,Wang, Jichao,Ni, Zhangqin,Wang, Sichang,Pan, Yuanjiang
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supporting information
p. 4582 - 4584
(2014/05/06)
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- Discovery of potent, selective, and orally bioavailable alkynylphenoxyacetic acid CRTH2 (DP2) receptor antagonists for the treatment of allergic inflammatory diseases
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New phenoxyacetic acid antagonists of CRTH2 are described. Following the discovery of a hit compound by a focused screening, high protein binding was identified as its main weakness. Optimization aimed at reducing serum protein binding led to the identification of several compounds that showed not only excellent affinities for the receptor (41 compounds with Ki 50 100 nM; PGD2-induced eosinophil shape change). Additional optimization of the PK characteristics led to the identification of several compounds suitable for in vivo testing. Of these, 19k and 19s were tested in two different pharmacological models (acute FITC-mediated contact hypersensitivity and ovalbumin-induced eosinophilia models) and found to be active after oral dosing (10 and 30 mg/kg).
- Crosignani, Stefano,Prêtre, Adeline,Jorand-Lebrun, Catherine,Fraboulet, Ga?le,Seenisamy, Jeyaprakashnarayanan,Augustine, John Kallikat,Missotten, Marc,Humbert, Yves,Cleva, Christophe,Abla, Nada,Daff, Hamina,Schott, Olivier,Schneider, Manfred,Burgat-Charvillon, Fabienne,Rivron, Delphine,Hamernig, Ingrid,Arrighi, Jean-Fran?ois,Gaudet, Marilène,Zimmerli, Simone C.,Juillard, Pierre,Johnson, Zoe
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experimental part
p. 7299 - 7317
(2011/12/15)
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- NAPHTHYLACETIC ACIDS
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The invention is concerned with the compounds of formula I: and pharmaceutically acceptable salts and esters thereof, wherein W, X, Y, and R1-R7 are defined in the detailed description and claims. In addition, the present invention relates to methods of manufacturing and using the compounds of formula I as well as pharmaceutical compositions containing such compounds. The compounds of formula I are antagonists or partial agonists at the CRTH2 receptor and may be useful in treating diseases and disorders associated with that receptor such as asthma.
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Page/Page column 31
(2010/06/13)
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- PHENOXY ACETIC ACID DERIVATIVES
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The present invention provides phenoxyacetic acid derivatives of Formula (I) for the treatment of CRTH2 related disorders and disease selected from asthma, atopic dermatitis and inflammatory dermatoses.
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Page/Page column 120
(2010/09/03)
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- ARYLALKYLAMINES AND PROCESS FOR PRODUCTION THEREOF
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The present invention relates to an arylalkylamine compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, a process for preparing the same, and use of the above-mentioned compound as an activating compound (CaSR agonist) of a Ca sensiing receptor, a pharmaceutical composition containing the above-mentioned compound as an effective ingredient, etc. The symbols in the formula represent the following meanings: Ar: optionally substituted aryl or optionally substituted heteroaryl here, the cyclic portion of the heteroaryl is bicyclic heterocyclic ring in which 5- to 6-membered monocyclic heterocyclic ring containing 1 or 2 hetero atom(s) and benzene ring are fused; R 1 : a group selected from the group consisting of optionally substituted cyclic hydrocarbon group, and optionally substituted heterocyclic group; n: an integer of 1 to 3; X: single bonding arm, -CH 2 -, -CO- , - (CH 2 ) m -CO- , -CH (R 2 ) -CO-, - (CH 2 ) p -Y-(C(R 3 ) (R 4 )) q -CO-, -NH-CO- or -N(R 5 ) -CO-; in the above-mentioned respective definitions of the X, the bonding arm described at the left end represents a bond with R 1 ; m is an integer of 1 to 3; p is an integer of 0 to 2; q is an integer of 0 to 2; Y: -O- or -SO 2 -; R 2 : phenyl or lower alkyl; R 3 , R 4 : each independently represents hydrogen atom or lower alkyl; R 5 : lower alkyl; provided that the ring portion of the group represented by R 1 is neither naphthylidine nor partially saturated group thereof, and, when X is -CH 2 - or -CO-, R 1 is not naphthyl.
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Page/Page column 31
(2010/11/25)
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- PHENOXIACETIC ACID DERIVATIVES
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The invention relates to certain 2-substituted phenoxyacetic acid derivatives of formula (I), in which the variables are as defined in the claims, useful in the treatment of diseases or conditions in which modulation of the CRTh2 receptor is beneficial, s
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Page/Page column 49
(2008/06/13)
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- DIPEPTIDYL PEPTIDASE IV INHIBITOR
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A compound represented by general formula (I):A-B-D whereinA represents a substituted or unsubstituted 1-pyrrolidinyl group, a substituted or unsubstituted 3-thiazolidinyl group, a substituted or unsubstituted 1-oxo-3-thiazolidinyl group, or the like;B r
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Page/Page column 85
(2010/11/29)
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- Diaminopyrimidines
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Substituted-phenyl derivatives of 5-(1,4-piperazinyl)-2,4-pyrimidinediamine are effective as antibacterial and antitumor agents. Methods of preparing such compounds, pharmaceutical compositions based thereon, and a method of treating bacterial infections in a mammal in need of such treatment are disclosed.
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