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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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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

 

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

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Scandium-Catalyzed para-Selective Alkylation of Aromatic Amines with Alkenes

An efficient para-alkylation of primary and secondary anilines with a variety of sterically encumbered alkenes using a simple beta-diketiminato scandium catalyst is reported. This protocol features 100% atom economy, excellent chemo- and regioselectivity, broad substrate scope, and good functional group tolerance. Mechanistic studies disclosed that the reaction probably proceeded via a tandem hydroamination/Hofmann-Martius rearrangement.

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

 

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BENZOXAZINES, BENZOTHIAZINES, AND RELATED COMPOUNDS HAVING NOS INHIBITORY ACTIVITY

The present invention features benzoxazines, benzothiazines, and related compounds that inhibit nitric oxide synthase (NOS), particularly those that selectively inhibit neuronal nitric oxide synthase (nNOS) in preference to other NOS isoforms. The NOS inhibitors of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing various medical conditions

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

 

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7-fused 2-(piperazinoalkyl) indole derivatives, intermediates and compositions thereof

Pharmacologically active compounds having anti-allergic properties corresponding to the formula I STR1 which can be mono- or disubstituted in the phenyl ring and their acid addition salts and/or S-mono- or dioxides of sulfur-containing compounds of the formula I are described, together with processes and intermediates for their preparation.

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

 

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A review on synthesis of benzothiazine analogues

Scientific advances mainly involves the development of new and highly reactive compounds. Nitrogen and sulphur containing benzothiazines forms highly active heterocyclic agents. Benzothiazines are prominent class of heterocyclic compound. Many studies have been done in the development of benzothiazine analogues. Microwave assisted synthesis, regioselective techniques and other methods are also used for benzothiazine synthesis. Various methods have been developed for the synthesis of benzothiazine derivatives. Benzothiazines exhibits numerous therapeutic activities like anti-HIV, calcium antagonistic, anti-serotinin, analgesic, anti-mycobacterial anti-microbial, anti-oxidant, anti-rheumatic, anti-inflammatory, anti-hypertensive ,calcium channel blocker, anti-malarial, potassium channel opener, cardiovascular, anthelmintic, neuroprotective, aldose reductase inhibitor, herbicidal, pesticidal etc. This has raised the necessity to explore novel benzothiazine derivatives which can significantly contribute to the development of therapeutically active agents. And the newer development of novel benzothiazines derivatives also involves the same characteristic features and also contribute various activities.

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

 

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ORGANOMETALLIC INDUCED SELF-CONDENSATION OF CARBOXAMIDES

N,N-Disubstituted carboxamides containing alpha-hydrogen atoms undergo self-condensation reaction simply on treatment with Grignard reagents or n-BuLi in THF at room temp.The reaction is considerably influenced by steric hindrance at the alpha-carbon and the condensing agent utilized.A possible Claisen-type mechanism is also reported.

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

 

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TRICYCLIC INDOLE MCL-1 INHIBITORS AND USES THEREOF

The present invention provides for compounds that inhibit the activity of an anti-apoptotic Bcl-2 family member Myeloid cell leukemia-1 (Mcl-1) protein. The present invention also provides for pharmaceutical compositions as well as methods for using compounds for treatment of diseases and conditions (e.g., cancer) characterized by the over-expression or dysregulation of Mcl-1 protein.

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

 

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An efficient synthesis of benzene fused six-, seven- and eight-membered rings containing nitrogen and sulfur by benzyne ring closure reaction

3,4-Dihydro-2-H-benzo[1,4]thiazines (3a-c), 2,3,4,5-tetrahydro[b]-[1,4] thiazapines (3d-f) and 2,3,4,5-tetrahydro-2H-benzo[b][1,4]thiazocines (3g-i) were prepared by the cyclization of the respective 2-bromophenylsulfanyl derivatives of ethylamine (1a-c), propylamine (2d-f) and butylamine (2g-i).

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

 

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1-PROPANOL AND 1-PROPYLAMINE DERIVATIVES AND THEIR USE AS GLUCOCORTICOID LIGANDS

Compounds of Formula (I) wherein R1, R2 R3, R4, R5, R6, and X are as defiend herein for Formula (IA) and Formula (IB), or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocoricoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.

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