cas 153435-79-1, 3-BROMO-N-METHYLBENZENESULPHONAMIDE

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Copper-catalyzed oxidative methylation of sulfonamides by dicumyl peroxide
A novel and facile copper-catalyzed methylation of sulfonamides was herein demonstrated. The practical transformation took place readily under the oxidative conditions, and N-methyl amides (23 examples) were successfully furnished in high efficiency (up to 90% yields). Dicumyl peroxide was considered to act not only as the oxidant in the system, but also methyl donor for the methylation protocol.
Che, Shiying,Zhu, Qiao,Luo, Zhenghong,Lian, Yan,Zhao, Zijian
p. 935 - 942
(2021/01/05)

N-Methylation of Amines with Methanol in the Presence of Carbonate Salt Catalyzed by a Metal-Ligand Bifunctional Ruthenium Catalyst [(p-cymene)Ru(2,2′-bpyO)(H2O)]
A ruthenium complex [(p-cymene)Ru(2,2′-bpyO)(H2O)] was found to be a general and efficient catalyst for the N-methylation of amines with methanol in the presence of carbonate salt. Moreover, a series of sensitive substituents, such as nitro, ester, cyano, and vinyl groups, were tolerated under present conditions. It was confirmed that OH units in the ligand are crucial for the catalytic activity. Notably, this research exhibited the potential of metal-ligand bifunctional ruthenium catalysts for the hydrogen autotransfer process.
Liu, Peng,Tung, Nguyen Thanh,Xu, Xiangchao,Yang, Jiazhi,Li, Feng
p. 2621 - 2631
(2021/02/27)

Structure-activity relationship studies for the development of inhibitors of murine adipose triglyceride lipase (ATGL)
High serum fatty acid (FA) levels are causally linked to the development of insulin resistance, which eventually progresses to type 2 diabetes and non-alcoholic fatty liver disease (NAFLD) generalized in the term metabolic syndrome. Adipose triglyceride lipase (ATGL) is the initial enzyme in the hydrolysis of intracellular triacylglycerol (TG) stores, liberating fatty acids that are released from adipocytes into the circulation. Hence, ATGL-specific inhibitors have the potential to lower circulating FA concentrations, and counteract the development of insulin resistance and NAFLD. In this article, we report about structure–activity relationship (SAR) studies of small molecule inhibitors of murine ATGL which led to the development of Atglistatin. Atglistatin is a specific inhibitor of murine ATGL, which has proven useful for the validation of ATGL as a potential drug target.
Breinbauer, Rolf,Doler, Carina,Fuchs, Elisabeth,Grabner, Gernot F.,Mayer, Nicole,Melcher, Michaela-Christina,Migglautsch, Anna K.,Romauch, Matthias,Schweiger, Martina,Zechner, Rudolf,Zimmermann, Robert
supporting information

(2020/07/13)

Method for preparing TNNI3K inhibitor (by machine translation)
The method TNNI3K comprises the following steps: heating the m-bromobenzene sulfonamide in the presence of an iridium complex catalyst and a base: for a few hours and then cooling to room temperature, to dry the solvent, to obtain, methyl - 3 3-aminobenze
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Paragraph 0022-0027

(2020/03/12)

Synthetic TNNI3K inhibitors (by machine translation)
The invention discloses a method for synthesizing TNNI3K inhibitors, proceeding from interval tetrabromobensoate sulfonamides, containing double-imidazole ligand iridium complex and under the action of the weak catalytic activation methanol instead of high toxicity halogenated methane get methylation product, further with the ammonia generating uhlmann coupling reaction, the final with 4 - chloro-pyrrolo pyrimidine nucleophilic substitution reaction to obtain TNNI3K inhibitors. The present invention through the use of iridium metal complex as the methylation reaction catalyst, the reaction conditions are more moderate and high yield, without the need of high temperature and high pressure, nitrogen protection, severe conditions such as the reaction for a long time, the last step nucleophilic substitution reaction we adopt a microwave reactor greatly shorten the reaction time. (by machine translation)
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Paragraph 0035-0040

(2019/03/26)

COMPOUND HAVING γ TURN STRUCTURE AND LSD1 INHIBITOR USING THE SAME
PROBLEM TO BE SOLVED: To provide a compound having LSD1 inhibitory activity and cancer cell growth inhibitory effect. SOLUTION: There is provided a compound represented by the formula (1) and a salt thereof. (1), where R1 is an alkyl group, a cycloalkyl group, an aralkyl group, an aryl group or a heteroaryl group, R2 is H, an alkyl group, a cycloalkyl group, an aryl group or a heteroaryl group, R3 is H, an alkyl group, a cycloalkyl group, an aralkyl group, an aryl group or a heteroaryl group, R4 is an aryl group or a heteroaryl group, each of the above described groups may be substituted, n is an integer of 2 to 10 and *1 and *2 are asymmetric carbons. SELECTED DRAWING: None COPYRIGHT: (C)2018,JPO&INPIT
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Paragraph 0377-0382

(2017/12/27)

N-Methylation of Amines with Methanol Catalyzed by a Cp?Ir Complex Bearing a Functional 2,2′-Bibenzimidazole Ligand
A new type of Cp?Ir complex bearing a functional 2,2′-bibenzimidazole ligand was designed, synthesized, and found to be a highly effective and general catalyst for the N-methylation of a variety of amines with methanol in the presence of a weak base (0.3 equiv of Cs2CO3).
Liang, Ran,Li, Shun,Wang, Rongzhou,Lu, Lei,Li, Feng
supporting information
p. 5790 - 5793
(2017/11/10)

C-H activation enables a rapid structure-activity relationship study of arylcyclopropyl amines for potent and selective LSD1 inhibitors
We describe the structure-activity relationship of various arylcyclopropylamines (ACPAs), which are potent LSD1 inhibitors. More than 45 ACPAs were synthesized rapidly by an unconventional method that we have recently developed, consisting of a C-H borylation and cross-coupling sequence starting from cyclopropylamine. We also generated NCD38 derivatives, which are known as LSD1 selective inhibitors, and discovered a more effective inhibitor compared to the original NCD38.
Miyamura, Shin,Araki, Misaho,Ota, Yosuke,Itoh, Yukihiro,Yasuda, Shusuke,Masuda, Mitsuharu,Taniguchi, Tomoyuki,Sowa, Yoshihiro,Sakai, Toshiyuki,Suzuki, Takayoshi,Itami, Kenichiro,Yamaguchi, Junichiro
p. 8576 - 8585
(2016/09/28)

2,7-SUBSTITUTED THIENO[3,2-D] PYRIMIDINE COMPOUNDS AS PROTEIN KINASE INHIBITORS
Disclosed are a 2,7-substituted thieno[3,2-d]pyrimidine compound having a protein kinase inhibition activity, a pharmaceutically acceptable salt, and a pharmaceutical composition for prevention and treatment of diseases caused by abnormal cell growth comp
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Page/Page column 18

(2012/11/08)

2,7-SUBSTITUTED THIENO[3,2-D]PYRIMIDINE COMPOUNDS AS PROTEIN KINASE INHIBITORS
Disclosed are a 2,7-substituted thieno[3,2-d]pyrimidine compound having a protein kinase inhibition activity, a pharmaceutically acceptable salt, and a pharmaceutical composition for prevention and treatment of diseases caused by abnormal cell growth comp
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Page/Page column 38

(2011/05/06)

CARBOXYLIC DERIVATIVES FOR USE IN THE TREATMENT OF CANCER
The invention provides novel compounds of formula (I), wherein: R1 is a radical derived from one of the known ring systems; R2 is a phenyl radical optionally substituted; Xn represents a birradical selected from the group consisting of: -(CH2)1-4-, (C2-C4)-alkenyl, (C2-C4)alkynyl, -S-(CH2)1-3-#, and -(CH2)1-3-O-#; wherein the symbol # indicates the position at which Xn is attached to R1; Yn is a birradical selected from the group consisting of: -(CH2)2-4-, -S-(CH2)1-3#, and -O-(CH2)1-3-#,; where in the symbol # indicates the position at which Yn is attached to R2; and R3 is a radical selected from the group consisting of: -OR4. The compounds of formula (I) are useful in the treatment of cancer
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Page/Page column 65

(2009/07/25)

NOVEL QUINAZOLINES AS 5-HT6 MODULATORS II
The present invention relates to new compounds of formula I, or salts, solvates or solvated salts thereof, wherein Q, B, R1, R2, R3, R4, m and n are defined as in claim 1, processes for their preparation and to
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Page/Page column 41

(2010/11/28)

SPIROPIPERIDINE COMPOUNDS USEFUL AS BETA-SECRETASE INHIBITORS FOR THE TREATMENT OF ALZHERMER’S DISEASE
The present invention is directed to spiropiperidine compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. T
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Page/Page column 128

(2010/11/08)

Acetylenyl-pyrazolo-pyrimidine derivatives
The present invention relates to compounds of formula (I): wherein R1 to R3, A, M, L, E, G, and J are as defined in the description and claims. The invention also relates to a process for the manufacture of such compounds, pharmaceutical compositions containing them, and methods for treating CNS disorders.
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Page/Page column 29

(2008/06/13)

OMEGA-CARBOXYARYL SUBSTITUTED DIPHENYL UREAS AS RAF KINASE INHIBITORS
This invention relates to the use of a group of aryl ureas in treating raf mediated diseases, and pharmaceutical compositions for use in such therapy.
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Page/Page column 15

(2010/01/31)

Omega-carboxyaryl substituted diphenyl ureas as raf kinase inhibitors
This invention relates to the use of a group of aryl ureas in treating raf mediated diseases, and pharmaceutical compositions for use in such therapy.
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(2008/06/13)

omega-carboxyaryl substituted diphenyl ureas as raf kinase inhibitors
This invention relates to the use of a group of aryl ureas in treating raf mediated diseases, and pharmaceutical compositions for use in such therapy.
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(2008/06/13)

Inhibition of RAF kinase using quinolyl, isoquinolyl or pyridyl ureas
This invention relates to the use of a group of aryl ureas in treating raf mediated diseases, and pharmaceutical compositions in such therapy.
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(2008/06/13)

Omega-carboxyaryl subsituted diphenyl ureas as raf kinase inhibitors
This invention relates to the use of a group of aryl ureas in treating raf mediated diseases, and pharmaceutical compositions for use in such therapy.
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(2008/06/13)

Pyridine derivatives and pharmaceutical compositions containing them
The invention relates to novel pyridyl derivatives, their use as medicaments, pharmaceutical formulations containing them and methods for their preparation.
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(2008/06/13)

Compounds
A compound of formula I,wherein- X represents (CH2)n O, (CH2)n S or C2 alkylene;n represents 1 or 2; Ar1 represents indanyl, tetrahydronaphthyl, naphthyl or phenyl, which latter two groups may be substituted by one or more substituents selected from chloro, fluoro, OR1, O(CH2)m CONR20R21, C(O)R2, C1-6 alkyl (optionally substituted by one or more fluorine atoms), pyridyl, thiazinyl, phenyl or C7-9 alkylphenyl which latter two groups are optionally substituted by one or more substituent selected from halo, nitro, OR3, C1-6 alkyl (optionally substituted by one or more fluorine atoms), C(O)R4, C(O)OR5, C(O)N(R6)R7, CN, CH2OR14, CH2NR15R16, N(R8)R9, N(R10)SO2R11, N(R12)C(O)R13, OC(O)R19 and SO2NR17R18; m represents an integer 1 to 3; R1, R2 and R3 independently represent H, C1-10 alkyl (optionally substituted by one or more fluorine atoms), C7-9 alkylphenyl or phenyl, which latter group is optionally substituted by hydroxy; and R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, R18, R19, R20 and R21 independently represent H, C1-6 alkyl (optionally substituted by one or more fluorine atoms) or phenyl; in which any alkyl group present may be interrupted by one or more oxygen atoms; provided that when X represents CH2CH2, Ar1 may not represent phenyl or phenyl substituted with one or more substituents OR1, in which R1 represents C1-10 alkyl; or a pharmaceutically acceptable derivative thereof, may be used for the treatment of a reversible obstructive airways disease or allergic conditions of the skin, nose and eye
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(2008/06/13)

EFFECT OF STRUCTURE ON THE KINETICS AND MECHANISM OF THE ACID-CATALYZED DECOMPOSITION OF N-ALKYL-N-NITROBENZENESULFONAMIDES
The decomposition rate of a series of meta- and para-substituted N-alkyl-N-nitrobenzenesufonamides was determined by a spectrophotometric method in aqueous sulfuric acid.It was shown that the decomposition of the compounds takes place both by denitration and by cleavage of the N-S bond with the formation fo primary aliphatic N-nitrosamines.Electron-withdrawing substituents in the aromatic ring shift the process toward denitration.
Drozdova, O. A.,Astrat'ev, A. A.,Kuznetsov, L. L.,Selivanov, V. F.
p. 671 - 675
(2007/10/02)