66176-39-4Relevant academic research and scientific papers
Preparation method of substituted benzene sulfonyl chloride
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Paragraph 0051-0054, (2021/05/08)
The invention provides a preparation method of substituted benzene sulfonyl chloride, which comprises the following steps: carrying out diazotization reaction on an aniline compound with a structure as shown in a formula I to obtain fluoboric acid diazonium salt with a structure as shown in a formula II; obtaining substituted benzene sulfonyl chloride with a structure as shown in a formula III from the fluoboric acid diazonium salt with the structure as shown in the formula II; wherein R is selected from any one of ortho-chlorine, bromine, methyl, chloromethyl, bromomethyl, nitro, cyano, acetyl, meta-chlorine, bromine, methyl, chloromethyl, bromomethyl, nitro, cyano, acetyl, para-chlorine, bromine, methyl, chloromethyl, bromomethyl, nitro, cyano and acetyl. The preparation method of the substituted benzene sulfonyl chloride provided by the invention is simple in reaction process, easy to operate, ideal in effect and suitable for industrial production.
An in situ combinatorial methodology to synthesize and screen chemical probes
Van Der Zouwen, Antonie J.,Lohse, Jonas,Wieske, Lianne H. E.,Hohmann, Katharina F.,Van Der Vlag, Ramon,Witte, Martin D.
supporting information, p. 2050 - 2053 (2019/02/19)
Chemical probes that label proteins of interest in the context of complex biological samples are useful research tools. The reactive group that forms the covalent bond with the target protein has a large effect on the selectivity and selecting the appropriate group determines the success of a probe. We here report the development of a combinatorial methodology based on imine chemistry that enables straightforward in situ synthesis and screening of different reactive groups and thereby simplifies identification of probe leads. Using our methodology, we found chemical probes targeting BirA and chloramphenicol acetyl transferase, two proteins associated with antibacterial activity and resistance.
Carbocation Catalyzed Bromination of Alkyl Arenes, a Chemoselective sp3 vs. sp2 C?H functionalization.
Ni, Shengjun,El Remaily, Mahmoud Abd El Aleem Ali Ali,Franzén, Johan
supporting information, p. 4197 - 4204 (2018/09/25)
The versatility of the trityl cation (TrBF4) as a highly efficient Lewis acid organocatalyst is demonstrated in a light induced benzylic brominaion of alkyl-arenes under mild conditions. The reaction was conducted at ambient temperature under common hood light (55 W fluorescent light) with catalyst loadings down to 2.0 mol% using N-bromosuccinimide (NBS) as the brominating agent. The protocol is applicable to an extensive number of substrates to give benzyl bromides in good to excellent yields. In contrast to most previously reported strategies, this protocol does not require any radical initiator or extensive heating. For electron-rich alkyl-arenes, the trityl ion catalyzed bromination could be easily switched between benzylic sp3 C?H functionalization and arene sp2 C?H functionalization by simply alternating the solvent. This chemoselective switch allows for high substrate control and easy preparation of benzyl bromides and bromoarenes, respectively. The chemoselective switch was also applied in a one-pot reaction of 1-methylnaphthalene for direct introduction of both sp3 C?Br and sp2 C?Br functionality. (Figure presented.).
Synthesis of novel N-(2-Hydroxyphenyl)arylsulfonamides as selective HDAC inhibitory and cytotoxic agents
Kim, Jungsu,Chun, Pusoon,Moon, Hyung Ryong
, p. 1487 - 1493 (2013/07/28)
Based on the finding that the 2-aminobenzamido group of MS-275 plays a crucial role in inhibiting HDACs through chelation of zinc existing at the active site of HDAC enzymes, novel N-(2-hydroxyphenyl)aryl-sulfonamide derivatives were synthesized for their potential ability to inhibit HDACs and evaluated for anticancer activity against human breast cancer cell line (MCF-7). Although the synthesized arylsulfonamides have failed to significantly inhibit total HDACs activity, phenyl carbamate-linked arylsulfonamide 10 and benzyl thiocarbamate-linked arylsulfonamide 15 exhibited good anticancer activities, which were only 4.3- and 3.6-fold lower anticancer activities, respectively, than MS-275 that is undergoing phase II clinical trials. These results suggest that these compounds may act as a selective HDAC inhibitor and probably N-(2-hydroxy-phenyl)sulfamoyl group may play an important role in interacting with HDAC enzymes through chelation of zinc ion.
4-PHENYL-5-OXO-1,4,5,6,7,8-HEXAHYDROQUINOLINE DERIVATIVES THE TREATMENT OF INFERTILITY
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Page/Page column 53, (2010/11/24)
The present invention relates to 4-phenyl-5-oxo-l,4)5,6,7,8-hexahydroquinoline derivatives according to Formula I, Formula I or a pharmaceutically acceptable salt thereof, wherein R1 is (l-6C)alkyl, (2-6C)alkenyl or (2-6C)aDcynyl; R2, R3 are independently halogen, (l-4C)allcyl, (2-4C)alkenyl, (2-4C)- alkynyl, (1 -4C)aBcoxy, (3-4C)alkenyloxy or (3-4C)alkynyloxy; R4 is phenyl or (2-5C)- heteroaryl, both substituted with R7 and optionally substituted on the (hetero)aromatic ring with one or more substituents selected from hydroxy, amino, halogen, nitro, trifluoromethyl, cyano, (l-4C)alkyl, (l-4C)alkoxy , (l-4C)alkylthio and (di)(l-4C)- alkylamino. The invention also relates to pharmaceutical compositions comprising said derivatives, as well as to the use of these 4-phenyl-5-oxo-l, 4,5,6, 7,8-hexahydro- quinoline derivatives in therapy, more specifically for the treatment of infertility
Heterocyclic sulfonamide derivatives as antagonists of PAF and angiotensin II
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, (2008/06/13)
Compounds of formula (I), wherein: A represents: a) a --VR6 group wherein v is --C(=O), --C(=O)O--, --CH2 O--, --CH2 OC(=O)--, --C(=S)--, --CH2 OC(=O)NH--, --C(=S)O--, --CH2 S--, --C(=O)NHSO2 --, --SO2 NHC(=O)-- or --CH2 OSiPh2 --; b) a --CH2 NR9 R10 group or a --CONR9 R10 group wherein each of R9 and R10 is independently hydrogen, -alkyl-, -alkenyl-, -alkynyl, -cycloalkyl, -cycloalkenyl, pyridyl (any of which may optionally be substituted) or a group --D as defined above or R9 and R10 together with the nitrogen atom to which they are attached form a nitrogen-containing heterocyclic ring; c) a group Y where Y is a 5- or 6-membered optionally substituted heterocyclic ring containing one or more heteroatoms selected from nitrogen, oxygen and sulphur; or d) a group --CH2 Y or --C(=O)NHY; where Y is as defined above; B represents a 5- or 6-membered heterocyclic ring containing one or more nitrogen atoms in its ring, are antagonists of platelet activating factor (PAF) and/or antagonists of angiotensin II.
4-(1H-2-methylimidazo[4,5-c]pyridinylmethyl)phenylsulphonamide derivatives as antagonist of PAF
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, (2008/06/13)
The present invention is directed to compounds of general formula I as well their pharmaceutically and veterinarily acceptable acid addition salts or hydrates thereof. The present invention is further directed to pharmaceutical and veterinary compositions containing the compounds of general formula I. The present compounds of general formula I are antagonist of platelet activating factor (PAF). Accordingly, the present invention is also directed to methods for preventing, treating or ameliorating in human or mammalian animals, various diseases or physiological conditions mediated by PAF.
Imidazo (4,5-C) pyridine derivatives as PAF antagonists
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, (2008/06/13)
Compounds of formula I: STR1 wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, and B are variables. These compounds are antagonists of platelet activating factor (PAF) and as such are useful in the treatment or amelioration of various diseases or disorders mediated by PAF.
Sulphonylbenzyl-substituted imidazoles
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, (2008/06/13)
Sulphonylbenzyl-substituted imidazoles can be prepared by first reacting imidazolylaldehydes with sulphonylbenzyl compounds and then oxidising or reducing the aldehyde function in the customary manner. The sulphonylbenzyl-substituted imidazoles can be used as active compounds in medicaments.
Sulphonylbenzyl-substituted imidazopyridines
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, (2008/06/13)
Sulphonylbenzyl-substituted imidazopyridines can be prepared by reacting correspondingly substituted imidazopyridines with sulphonylbenzyl compounds. The sulphonylbenzyl-substituted imidazopyridines can be employed as active compounds in medicaments, in particular for the treatment of hypertension and atherosclerosis.
