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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

 

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An Easy and Efficient Synthesis of 4H-Thiazolo<5,4,3-i,j>quinolin-4-ones and 5H-1,4-thiazino<2,3,4-i,j>quinolin-5-ones

The title heterocycles have been synthesized by a Claisen-type self condensation of acetylbenzothiazolines and acetyldihydrobenzothiazines and subsequent cyclization.

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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. Recommanded Product: 3,4-Dihydro-2H-benzo[b][1,4]thiazine

COMPOUND HAVING 11 beta HSD1 INHIBITORY ACTIVITY

The present invention provides compounds having excellent 11-HSD1 inhibitory activity. A compound represented by the following formula (I): [wherein X 1 represents an oxygen atom, or the formula -(CR 11 R 12 ) p -, etc., Y 1 represents a hydrogen atom, a hydroxyl group, etc., Z 1 represents an oxygen atom or the formula -(NR 14 )-, R 1 represents a hydrogen atom, a halogen atom, a cyano group, a C 1-4 alkyl group, a C 1-4 alkyl group substituted with 1 to 3 halogen atoms, a C 1-4 alkoxy group, a C 1-4 alkoxycarbonyl group, a carboxyl group, a carbamoyl group, or an amino group, and m represents an integer of 1 or 2, and R 2 represents a hydrogen atom or a C 1-4 alkyl group, and n represents an integer of 1 or 2]

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

 

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Biotransformation of organic sulfides. Part 12. Conversion of heterocyclic sulfides to chiral sulfoxides by Helminthosporium sp. NRRL 4671 and Mortierella isabellina ATCC 42613

The enantioselective oxidation of a series of heterocyclic prochiral sulfides to chiral sulfoxides has been examined using the fungal biocatalysts Helminthosporium species NRRL 4671 and Mortierella isabellina ATCC 42613. Methylthiofuranyl and -thiophenyl substrates gave (S)-configuration products in low to moderate enantiomeric purity on biotransformation with H. species, but pyridyl sulfides with the nitrogen atom located at an optimal distance of 8-10 A from the sulfur centre gave (S) sulfoxides of high enantiomeric purity. The biotransformation of appropriately substituted benzothiane substrates by M. isabellina also gave products of high enantiomeric purity, but with (R) configuration at sulfur. The acceptability of the substrate and the configuration of sulfur oxidation by both H. species and M. isabellina for the range of substrates examined were found to be consistent with predictions based on cubic space models for these oxidations.

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

 

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Design, synthesis, and antidiabetic activity of 4-phenoxynicotinamide and 4-phenoxypyrimidine-5-carboxamide derivatives as potent and orally efficacious TGR5 agonists

4-Phenoxynicotinamide and 4-phenoxypyrimidine-5-carboxamide derivatives as potent and orally efficacious TGR5 agonists are reported. Several 4-phenoxynicotinamide derivatives were found to activate human and mouse TGR5 (hTGR5 and mTGR5) with EC50 values in the low nanomolar range. Compound 23g, with an EC50 value of 0.72 nM on hTGR5 and an EC 50 value of 6.2 nM on mTGR5, was selected for further in vivo efficacy studies. This compound exhibited a significant dose-dependent glucagon-like peptide-1 (GLP-1) secretion effect. A single oral dose of 23g (50 mg/kg) significantly reduced blood glucose levels in db/db mice and caused a 49% reduction in the area under the blood glucose curve (AUC)0-120min following an oral glucose tolerance test (OGTT) in imprinting control region (ICR) mice. However, 23g stimulated gallbladder filling, which might result in side effects to the gallbladder.

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

 

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An efficient method for the N-formylation of amines under catalyst- and additive-free conditions

A simple catalyst- and additive-free method for the N-formylation of amines has been developed. The advantages of this protocol include a wide range of functional group tolerance, high efficiency and a lack of required extra promoters under mild conditions. This convenient strategy will provide a facile synthesis towards N-formamide natural products and pharmaceutical derivatives. A mechanism that involves difluorocarbene is proposed for this reaction.

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

 

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Copper-Catalyzed N-Formylation of Amines through Tandem Amination/Hydrolysis/Decarboxylation Reaction of Ethyl Bromodifluoroacetate

Ethyl bromodifluoroacetate (BrCF2COOEt) was first used as the N-formylating reagent in the copper-catalyzed N-formylation of amines. A range of primary, secondary, cyclic arylamines, and aliphatic amines underwent the N-formylation smoothly to furnish the N-formamides in moderate-to-excellent yields.

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

 

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HYDANTOINS AND RELATED HETEROCYCLES AS INHIBITORS OF MATRIX METALLOPROTEINASES AND/OR TNF-ALPHA CONVERTING ENZYME (TACE)

The present application describes novel hydantoin derivatives of formula (I): or pharmaceutically acceptable salt or prodrug forms thereof, wherein A, B, R1, R2, R3, R4, R5, R 6, R7, R11, and n 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.

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

 

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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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Efficient access to 1,4-benzothiazine: Palladium-catalyzed double C-S bond formation using Na2S2O3 as sulfurating reagent

A novel Pd-catalyzed double C-S bond formation coupling reaction has been developed. This protocol, in which Na2S2O3 was used as sulfurating reagent in metal-catalyzed reactions, provides an efficient method for the synthesis of substituted 1,4-benzothiazine derivates, which are structural elements of numerous bioactivity molecules rendering this protocol attractive to both synthetic and medicinal chemistry.

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