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A non-metal catalytic three-stage aromatic amide-way selective reduction of the new method (by machine translation)

The invention relates to a high efficiency, two-way selective tertiary aromatic amide and organic silicon reagent silicon hydrogenation reduction reaction green new method. Selecting non-metal catalytic system, under mild conditions can be successfully catalytic three-stage aromatic amide with low-cost of the peripheric (PHMS) or triethoxy silane to selective production of secondary or tertiary organic amine compound. The first time the use of organosilicon reagent breakthrough of electronic effect of steric differences and realize three-stage aromatic amide-way selective reduction reaction, is the reduction of amides and derivatives thereof provides a completely new strategy, also the method overcomes the prevailing poor substrate functional group compatibility, high costs of production and the like, industrial production or laboratory preparation amine compounds have provided broad prospects. (by machine translation)

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Reference£º
Thiazine – an overview | ScienceDirect Topics,
Thiazine | C4H5NS – PubChem

 

Discovery of 3,4-Dihydro-2H-benzo[b][1,4]thiazine

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REACTION BETWEEN N-ACYL-2,3-DIHYDROBENZO-1,4-THIAZINE AND N-ACYLPHENOTIAZINE WITH ORGANOMETALLIC REAGENTS

The title N-acyl-derivatives react with n-BuLi and Grignard reagents leading to products, which, formally, can be considered as derived from a Claisen-type condensation reaction.

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Reference£º
Thiazine – an overview | ScienceDirect Topics,
Thiazine | C4H5NS – PubChem

 

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Cyclic hydroxamic acids as inhibitors of matrix metalloproteinases and/or TNF-alpha converting enzyme (TACE)

The present application describes novel cyclic hydroxamic acids of formula I: 1or pharmaceutically acceptable salt forms thereof, wherein ring B is a 5-7 membered cyclic system containing from 0-2 heteroatoms selected from O, N, NR1, and S(O)p, and 0-1 carbonyl groups and the other variables are defined in the present specification, which are useful as inhibitors of matrix metalloproteinases (MMP), TNF-alpha converting enzyme (TACE), aggrecanase or a combination thereof, pharmaceutical compositions containing the same, and methods of using the same.

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Reference£º
Thiazine – an overview | ScienceDirect Topics,
Thiazine | C4H5NS – PubChem

 

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Sodium Triethylborohydride-Catalyzed Controlled Reduction of Unactivated Amides to Secondary or Tertiary Amines

The first transition-metal-free catalytic protocol for controlled reduction of amide functions using cheap and bench-stable hydrosilanes as reducing agents has been established. By altering the hydrosilane and solvent, the new method enables the selective cleavage of unactivated C-O bonds in amides and allows the C-N bonds to selectively break via the deacylated cleavage. Overall, this novel process may offer a versatile alternative to current methodologies employing stoichiometric metal systems for the controlled reduction of carboxamides.

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Reference£º
Thiazine – an overview | ScienceDirect Topics,
Thiazine | C4H5NS – PubChem

 

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Chemoselective Deprotection of Sulfonamides under Acidic Conditions: Scope, Sulfonyl Group Migration, and Synthetic Applications

Chemoselective acidic hydrolysis of sulfonamides with trifluoromethanesulfonic acid has been evaluated as a deprotection method and further extended to more complex synthetic applications. In contrast to conventional troublesome sulfonamide hydrolysis, a near-stoichiometric amount of acid was found to be sufficient to bring about efficient deprotection of various neutral or electron-deficient N-arylsulfonamides, whereas electron-rich substrates provided sulfonyl group migration products. The deprotection method developed is fully selective for N-arylsulfonamides, and the possibility to discriminate among various different sulfonamides is demonstrated.

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Reference£º
Thiazine – an overview | ScienceDirect Topics,
Thiazine | C4H5NS – PubChem

 

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Design of Gut-Restricted Thiazolidine Agonists of G Protein-Coupled Bile Acid Receptor 1 (GPBAR1, TGR5)

Bile acid signaling and metabolism in the gastrointestinal tract have wide-ranging influences on systemic disease. G protein-coupled bile acid receptor 1 (GPBAR1, TGR5) is one of the major effectors in bile acid sensing, with demonstrated influence on metabolic, inflammatory, and proliferative processes. The pharmacologic utility of TGR5 agonists has been limited by systemic target-related effects such as excessive gallbladder filling and blockade of gallbladder emptying. Gut-restricted TGR5 agonists, however, have the potential to avoid these side effects and consequently be developed into drugs with acceptable safety profiles. We describe the discovery and optimization of a series of gut-restricted TGR5 agonists that elicit a potent response in mice, with minimal gallbladder-related effects. The series includes 12 (TGR5 EC50: human, 143 nM; mouse, 1.2 nM), a compound with minimal systemic availability that may have therapeutic value to patients with type 2 diabetes mellitus, nonalcoholic steatohepatitis, or inflammatory bowel disease.

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Reference£º
Thiazine – an overview | ScienceDirect Topics,
Thiazine | C4H5NS – PubChem

 

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Preparation of potentially bioactive aza and thiaza polycyclic compounds containing a bridgehead nitrogen atom synthesis and antimicrobial activity of some pyrrolo[1,2,3-de]-1,4-benzothiazines

The synthesis of the 2,3-dihydro-pyrrolo[1,2,3-de]-1,4-benzothiazine 1a and 11b,12-dihydro-isoquino[1,2-c]-1,4-benzothiazine 8 has been accomplished by using a Bischler type cyclization of the N-(2,2-diethoxyethyl)-3,4-dihydro-2H-1,4-benzothiazines 3a and 3d, respectively. The new compounds 1a and 8 together with the known pyrrolobenzothiazines 1b,c and some their derivatives and intermediates of preparation were tested in vitro for their antimicrobial activity. Compound 1b was the most active against the Gram-positive Bacillus subtilis. Compound 7b showed interesting antifungal activity when tested against Saccharomyces cerevisiae.

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Reference£º
Thiazine – an overview | ScienceDirect Topics,
Thiazine | C4H5NS – PubChem

 

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Process for ortho-cyanation of phenols or phenylamines

A process for ortho-cyanation of phenols or phenylamines which comprises reacting a phenyl compound having hydroxy or optionally substituted amino or cyclic amino, of which ortho position is vacant, with trichloroacetonitrile, C1 -C5 alkyl thiocyanate or C6 -C12 aryl thiocyanate in the presence of a boron trihalide and treating the resultant product with an alkali is provided, and said process is useful in the synthesis of intermediates for medicinals or pesticides.

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Reference£º
Thiazine – an overview | ScienceDirect Topics,
Thiazine | C4H5NS – PubChem

 

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Iridium-catalyzed dehydrogenative alpha-Functionalization of (Hetero)aryl-Fused cyclic secondary amines with indoles

Herein, by employing dehydrogenation as a substrate-activating strategy, a new iridium-catalyzed direct alpha-functionalization of (hetero)aryl-fused cyclic secondary amines with indoles has been demonstrated, which proceeds with merits that include high step- and atom-efficiency, readily available feedstocks, a simple catalyst system, good functional group tolerance, and operational simplicity.

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Reference£º
Thiazine – an overview | ScienceDirect Topics,
Thiazine | C4H5NS – PubChem

 

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In homogeneous catalysis, the catalyst is in the same phase as the reactant. The number of collisions between reactants and catalyst is at a maximum.In a patent, 3080-99-7, name is 3,4-Dihydro-2H-benzo[b][1,4]thiazine, introducing its new discovery. COA of Formula: C8H9NS

The scandium rare earth catalyst in the alkylation reaction of the amine to the location in the application (by machine translation)

The present invention relates to rare earth catalyst in catalytic aromatic amine containing scandium para-selectivity of the alkylation reaction in the application, the structural formula of the scandium rare earth catalyst are as follows: Aromatic amine aromatic primary amine or aromatic secondary amine. The invention also discloses a method for alkylation of the amine of preparation method: formula (1) aromatic amines of the formula (2) of the olefin in the scandium rare earth under the action of catalyst, in organic solvent for 60 – 150 C lower reaction, to obtain the location of alkylated aromatic amine, the reaction route is as follows: Wherein R1 Hydrogen, aromatic itaconate C1 – C10 Alkyl; R2 Hydrogen, C1 – C4 Alkyl, C1 – C4 Alkoxy, aryl or halogen; and R2 Can not be substituted in the para position; X is methylene or sulfur atom, n1 for 0 – 4 in either a value; R3 For C1 – C20 Alkyl, aryl or R5 Through a number of methylene ring, the number of methylene n2 for 1 – 4 in either a value; R4 Hydrogen, C1 – C20 Alkyl, aryl, thienyl, benzofuranyl or substituted aryl group; R5 Hydrogen, methyl or methylene; R6 Is hydrogen. (by machine translation)

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Reference£º
Thiazine – an overview | ScienceDirect Topics,
Thiazine | C4H5NS – PubChem