149105-00-0

Upstream product

• 6933-10-4 amino-5-bromo-2-toluene 
• 124-63-0 methanesulfonyl chloride 

Downstream Products

• 1006380-18-2 N-(3-methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)methanesulfonamide 
• 1312099-10-7 N-(4-(4-bromo-2-formylthiophen-3-yl)-3-methylphenyl)methanesulfonamide 
• 1225338-76-0 N-(2-methyl-4'-phenoxybiphenyl-4-yl)methanesulfonamide 

Relevant academic research and scientific papers

Soft-Hard Acid/Base-Controlled, Oxidative, N-Selective Arylation of Sulfonanilides via a Nitrenium Ion

In iodine(III)-catalyzed, dehydrogenative arylations of sulfonanilides, the functionalization of C-C bonds is preferred over the functionalization of C-N bonds. Herein, an unprecedented N-selective arylation of sulfonanilides using soft-hard acid-base (SHAB) control by a nitrenium ion over a carbenium ion is reported. Treatment of sulfonanilides with iodine(III) led to the formation of nitrenium ions (soft), which preferentially react with biphenyls (soft) over bimesityl (hard) to generate C-N bonds. The iodine(III) was generated in situ by using PhI and mCPBA at room temperature.

Synthesis of CF3CH2-Containing Indolines by Transition-Metal-Free Aryltrifluoromethylation of Unactivated Alkenes

With an unactivated double bond as the radical acceptor, allyl amines underwent a metal-free trifluoromethylation/cyclization cascade with CF3SO2Na (Langlois' reagent), affording CF3CH2-containing indolines and tetrahydroisoquinolines, whose practical syntheses are significant challenges. This protocol features mild conditions, low cost, and a broad substrate scope.

Synthetic method of CF3-containing indoline and 1,2,3,4-tetrahydroisoquinoline

The invention discloses a synthetic method of CF3-containing indoline and 1,2,3,4-tetrahydroisoquinoline and relates to the technical field of compound synthesis. The synthetic method herein is basedon metal-free trifluoromethylation/cyclization free radical cascade reaction using a nonactive olefin dual-bond as a free radical receptor; the reaction aforementioned helps synthesize, in one step, CF3-containing indoline and 1,2,3,4-tetrahydroisoquinoline. The synthetic method herein has the significant advantages of mild conditions, good operational simplicity, low cost, wide substrate range, good exo selectivity and the like.

ANNELATED PYRROLES AND THEIR USE AS CRAC INHIBITORS

The invention relates to substituted bicyclic pyrroloheterocyclyl compounds of general formula (I), wherein A1 and A2 represent direct bond or C(=O), with the proviso that 0 or 1 of A1 and A2 represents C(=O); m and n independently denote 0, 1, 2 or 3, with the proviso that the sum [n + m] is 1, 2, 3 or 4; R1 denotes H, F, CI, Br, I, CN, CF3, CF2H, CFH2, CO2H, CO2R13, R13, OH. O-R13, NH2, N(H)R13, N(R13)2, R2 represents 0 to 4 substituents, each independently selected from F, CI, Br, CN. CF3, CF2H, CFH2, R13, OH, O-R13, NH2, N(H)R13 and N(R13)2; Ar1 represents phenyl or 5- or 6-membered heteroaryl, in each case unsubstituted or substituted with one, two, three or four substituents, independently selected from F, CI, Br, CN, CF3. CF2H, CFH2, R13 and O- R13; or C3-6-cycloalkyl or 3 to 7 membered heterocycloalkyl, in each case unsubstituted or mono- or polysubstituted; Ar2 represents phenyl or 5- or 6-membered heteroaryl, wherein said phenyl or said heteroaryl may be unsubstituted or mono- or polysubstituted and may be condensed with a 4-, 5-, 6-or 7- membered ring, being carbocyclic or heterocyclic, wherein said condensed ring may be saturated, partially unsaturated or aromatic and may be unsubstituted or mono- or polysubstituted; useful as ICRAC inhibitors, to pharmaceutical compositions containing these compounds and to these compounds for the use in the treatment and/or prophylaxis of diseases and/or disorders, in particular inflammatory diseases and/or inflammatory disorders.

FUSED HETEROCYCLIC COMPOUNDS AS ION CHANNEL MODULATORS

The present invention relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given b

1, 7-NAPHTHYRIDINE DERIVATIVES AS P38 MAP KINASE INHIBITORS

This invention is directed to new inhibitors of the p38 mitogen-activated protein kinas having the general formula (I) to processes for their preparation; to pharmaceutical compositions comprising them; and to their use in therapy.