34161-81-4

Upstream product

• 2941-78-8 2-Amino-5-methylbenzoic acid 
• 98-59-9 p-toluenesulfonyl chloride 
• 941-55-9 4-toluenesulfonyl azide 
• 1426922-36-2 N-[2-(4'-methylbenzenesulfonamido)-5-methylbenzoyl]-S-methyl-S-phenylsulfoximine 
• 99-04-7 m-Toluic acid 

Downstream Products

• 34161-85-8 N-(2-formyl-4-methylphenyl)-4-methylbenzenesulfonamide 
• 132354-03-1 (E)-N-<2-(2-methylsulphinyl-2-methylthiovinyl)-4-methylphenyl>toluene-4-sulphonamide 
• 132353-95-8 N-Allyl-N-[2-(1-chloro-2,2-bis-methylsulfanyl-vinyl)-4-methyl-phenyl]-4-methyl-benzenesulfonamide 
• 132354-04-2 methyl N-(2-methylthiocarbonylmethyl-4-methylphenyl)-N-(toluene-4-sulphonyl)-2-aminoacetate 
• 132353-94-7 [[2-(1-Chloro-2,2-bis-methylsulfanyl-vinyl)-4-methyl-phenyl]-(toluene-4-sulfonyl)-amino]-acetic acid methyl ester 
• 599-86-0 4-methyl-N-(4-methylphenyl)benzenesulfonamide 
• 1315477-58-7 5-methyl-3-phenyl-1-tosyl-1H-indole-2-carbaldehyde 
• 1315477-41-8 1-(5-methyl-2-(tosylamino)phenyl)-1-phenylprop-2-yn-1-ol 
• 28561-54-8 2-Benzoyl-4-methyl-N-(p-toluolsulfonyl)-anilid 

Relevant academic research and scientific papers

Late-Stage Amination of Drug-Like Benzoic Acids: Access to Anilines and Drug Conjugates through Directed Iridium-Catalyzed C?H Activation

The functionalization of C?H bonds, ubiquitous in drugs and drug-like molecules, represents an important synthetic strategy with the potential to streamline the drug-discovery process. Late-stage aromatic C?N bond–forming reactions are highly desirable, but despite their significance, accessing aminated analogues through direct and selective amination of C?H bonds remains a challenging goal. The method presented herein enables the amination of a wide array of benzoic acids with high selectivity. The robustness of the system is manifested by the large number of functional groups tolerated, which allowed the amination of a diverse array of marketed drugs and drug-like molecules. Furthermore, the introduction of a synthetic handle enabled expeditious access to targeted drug-delivery conjugates, PROTACs, and probes for chemical biology. This rapid access to valuable analogues, combined with operational simplicity and applicability to high-throughput experimentation has the potential to aid and considerably accelerate drug discovery.

INHIBITORS OF OPLOPHORUS LUCIFERASE-DERIVED BIOLUMINESCENT COMPLEXES

Compounds that may selectively inhibit Oplophorus luciferase-derived bioluminescent complexes, e.g., NanoBiT? bioluminescent complex, are disclosed as well as compositions and kits comprising the compounds, and methods of using the compounds. The compounds are of formula (I) wherein R1-R4 and p and q are as defined in the claims.

Method for Preparing Derivatives of Anthranilic acid and Anti-inflammatory Use Thereof

The present invention relates to a production method of anthranilic acid derivatives which reacts benzoic acid derivatives and phenylsulfonyl azide derivatives under the presence of a [IrCp*Cl_2]_2 catalyst; and relates to an anti-inflammatory use of the

Direct C-H amidation of benzoic acids to introduce meta- and para-amino groups by tandem decarboxylation

The Ir-catalyzed mild C-H amidation of benzoic acids with sulfonyl azides was developed to give reactions with high efficiency and functional-group compatibility. Subsequent protodecarboxylation of ortho-amidated benzoic acid products afforded meta- or para-substituted (N-sulfonyl)aniline derivatives, the latter being inaccessible by other C-H functionalization approaches. The decarboxylation step was compatible with the amidation conditions, enabling a convenient one-pot, two-step process. Without a trace: Carboxylic acids are used as traceless directing groups in the Ir-catalyzed direct C-H amidation of arenes with sulfonyl azides under mild conditions. The tandem protodecarboxylation of the ortho-amidated benzoic acid products afforded meta- or para-substituted (N-sulfonyl)anilines, which are difficult to obtain by other C-H functionalization approaches.

Sulfoximine directed intermolecular o-C-H amidation of arenes with sulfonyl azides

The Ru(II)-catalyzed intermolecular o-C-H amidation of arenes in N-benzoylated sulfoximine with sulfonyl azides is demonstrated. The reaction proceeds with broad substrate scope and tolerates various functional groups. Base hydrolysis of the amidation product provides the anthranilic acid derivatives and methylphenyl sulfoximine (MPS) directing group. This method is successfully employed for the synthesis of HMR 1766.

Metal-free synthesis of 1H-indole-2-carbaldehydes by N-iodosuccinimide- mediated cyclization of 1-(2′-anilinyl)prop-2-yn-1-ols in water. A formal synthesis of (R)-calindol

A N-iodosuccinimide (NIS)-mediated method to prepare 1H-indole-2- carbaldehydes efficiently from cycloisomerization of 1-(2-aminophenyl)prop-2-yn- 1-ols is described. The reaction is operationally straightforward and accomplished in good to excellent yiel

Copper(II) triflate-catalyzed intramolecular hydroamination of homoallylic amino alcohols as an expedient route to trans-2,5-dihydro-1H-pyrroles and 1,2-dihydroquinolines

A new efficient synthetic route to trans-2,5-dihydro-1H-pyrroles and 1,2-dihydroquinolines that relies on copper(II) triflate-catalyzed intramolecular hydroamination of homoallylic amino alcohols under mild and operationally straightforward conditions is

Acid Catalysed Reactions of Aryl Ketene Dithioacetal S-Oxides: Synthesis of Chloroketene Thioacetals and Thioesters

Aryl ketene dithioacetal S-oxides, on treatment with hydrochloric acid in dichloromethane, give chloroketene thioacetals.The same reaction in the presence of hydrogen sulphide gives S-methyl thioesters.