81589-32-4

Upstream product

• 55962-05-5 [N-(p-tolylsulfonyl)imino]phenyliodinane 
• 135-02-4 ortho-anisaldehyde 
• 21849-40-1 dibromamine-T 
• 46270-50-2 1-(2-methoxyphenyl)-2-nitroethan-1-one 
• 21615-34-9 2-Methoxybenzoyl chloride 
• 92755-81-2 N-bromo-p-toluenesulfonamide 
• 579-75-9 2-Methoxybenzoic acid 
• 41085-71-6 bromamine T 
• 38316-04-0 1-(2-methoxy-phenyl)-2-nitro-ethanol 
• 70-55-3 toluene-4-sulfonamide 
• 98-59-9 p-toluenesulfonyl chloride 
• 98-88-4 benzoyl chloride 
• 67-56-1 methanol 
• 6971-74-0 N-benzoyl-p-toluenesulfonamide 

Downstream Products

• 1043527-79-2 C₁₅H₁₄ClNO₃S 
• 1369576-88-4 3-methoxy-4'-methyl-N-(4-methylbenzenesulfonyl)biphenyl-2-carboxamide 
• 1638287-07-6 2,6-dimethoxy-N-(4-methylbenzenesulfonyl)benzenecarboxamide 
• 221667-31-8 N-{[4-(cyclopropylcarbamoyl)phenyl]sulfonyl}-2-methoxybenzamide 

Relevant academic research and scientific papers

Improvements of C-H Radio-Iodination of N-Acylsulfonamides toward Implementation in Clinics

An improved protocol to perform C-H radio-iodination is described. These new conditions allow rapid and clean formation of radio-iodinated N-acylsulfonamides using [125 I]NIS and catalytic amounts of palladium acetate and para-toluenesulfonic a

Ru(ii)-catalyzed allenylation and sequential annulation of: N -tosylbenzamides with propargyl alcohols

We hereby report Ru(ii)-catalyzed C(sp2)-H allenylation of N-tosylbenzamides to access multi-substituted allenylamides. Furthermore, the allenylamides were converted to the corresponding isoquinolone derivatives via base mediated annulation. The current protocol features low catalyst loading, mild reaction conditions, high functional group compatibility and desired scalability. The unique functionality of the afforded allenes allowed further transformations to expand the practicality of the protocol. This journal is

Preparation method of benzoylsulfamoyl benzamide and preparation intermediate

The invention provides a preparation method of benzoylsulfamoyl benzamide. The method comprises the following steps: reacting a sulfamoyl benzoic acid compound as shown in formula (I) with pivaloyl chloride so as to generate an anhydride compound as shown in formula (II), and reacting the anhydride compound with amine. In the formulas, R1 is hydrogen, halogen, a C1-10 alkyl group, a C1-10 alkoxy group, a C3-8 cycloalkyl group, a C3-8 cycloalkoxy group, a halogenated C1-10 alkyl group, a halogenated C1-10 alkoxy group, a halogenated C3-8 cycloalkyl group or a halogenated C3-8 cycloalkoxy group,and R2 and R3 each independently represent hydrogen, a C1-10 alkyl group, or a C3-8 cycloalkyl group. The invention also relates to compounds as shown in the formula (II) and application of the compounds as intermediates for the preparation of compounds as shown in formula (III).

Controllable construction of isoquinolinedione and isocoumarin scaffolds: Via RhIII-catalyzed C-H annulation of N -tosylbenzamides with diazo compounds

A highly efficient protocol for the synthesis of isoquinolinediones by RhIII-catalyzed C-H activation/annulation/decarboxylation of N-tosylbenzamides with diazo compounds is reported. The switchable synthesis of isocoumarins was also achieved successfully via C-H activation/annulation with slight modification of the reaction conditions. Importantly, the synthetic utility of this new reaction was further demonstrated in an atom-economical and operationally convenient total synthesis of a TDP2 inhibitor derivative from commercially available starting materials.

Formation of esters and amides via metal-free Csp2-Csp3 bond cleavage of α-nitro ketone: Mechanistic insight to the reaction pathway

A catalyst free protocol for hucleophilic Csp2-Csp3 bond cleavage of a-nitroketone has been achieved for the formation of C-O and C-N bond. A series of differently substituted a-nitroketones could be selectively cleaved and converted into corresponding esters and tosylamides in presence of alcohols and bromamine-T respectively. Mechanism of the C-C bond cleavage has been proposed by identifying different reaction intermediates using IR and NMR spectroscopic methods.

Palladium-Mediated Site-Selective C-H Radio-iodination

The palladium-mediated C-H radio-iodination of arenes using sodium iodide as the primary isotopic source is reported and performed without chemical know-how in 30 min and applied to the synthesis of complex radio-iodinated compounds of biological interest.

Heteroannulation enabled by a bimetallic Rh(III)/Ag(i) relay catalysis: Application in the total synthesis of aristolactam BII

A redox-neutral bimetallic Rh(iii)/Ag(i) relay catalysis allowed the efficient construction of 3-alkylidene isoindolinones and 3-alkylidene isobenzofuranones. The Rh(iii) catalyst was responsible for the C-H monofluoroalkenylation reaction, whereas the Ag(i) salt was an activator for the follow-up cyclization. The methodology developed was applied as a key step in the rapid total synthesis of the natural product aristolactam BII.

Unexpected C-C bond cleavage of α-nitroketone in the presence of TsNBr2: A new pathway for C-N bond formation

A new catalyst-free protocol for C-N bond formation via the cleavage of α-nitroketone has been developed. When α-nitroketones are treated with TsNBr2 in the presence of potassium carbonate, unexpected cleavage of C(O)-CHNO2 bond of α-nitroketone was observed followed by the formation of corresponding amide. Various nitroketones could be converted to corresponding amide using this procedure.

Formation of new C-O and C-N bonds via base promoted Csp2-Csp3 bond cleavage of α-nitro ketone

A catalyst free protocol has been developed for nucleophilic Csp2-Csp3 bond cleavage of α-nitroketone in the presence of potassium carbonate to create new C-O and C-N bonds. A series of different substituted α-nitroketones could be selectively cleaved and converted into corresponding esters and tosylamides in the presence of alcohols and bromamine-T, respectively.

Design of novel CSA analogues as potential safeners and fungicides

Study of safeners has been seldom reported in literature. In this work, a series of novel acylsulfamoylbenzamide analogues was designed and synthesized with newly developed safener cyprosulfamide (CSA) as the leading compound. The activity assay against the herbicide thiencarbazone-methyl (TCM) on maize revealed that fifteen compounds showed better protective effect than CSA on the fresh weight of aerial parts, twelve compounds exhibited better activity on the dry weight of aerial parts. Remarkably, two compounds (6Ih, 7II) had protective effect on the four aspects of TCM treated maize. Further antifungal assay showed their excellent activity against Physollospora piricola. The structure-activity relationships of CSA analogues as safeners and fungicides were discussed and it might be valuable for further molecular modification of new CSA analogues.