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NHC-Catalyzed intramolecular redox amidation for the synthesis of functionalized lactams

A very efficient NHC-catalyzed lactamization reaction is reported. For most cases, the ring expansion reaction proceeds to cleanly furnish five- and six-membered N-Ts and N-Bn lactams, without the need for further purification. Evidence is presented suggesting a dual role for the stoichiometric base: (1) deprotonation of the triazolium precatalyst and (2) activation of the nitrogen leaving group through hydrogen bonding.

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Reference:
Oxazolidine – Wikipedia,
Oxazolidine | C3H1050NO – PubChem

 

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Challenges and approaches in the discovery of human immunodeficiency virus type-1 non-nucleoside reverse transcriptase inhibitors

The type I human immunodeficiency virus (HIV-1) pandemic affecting over 37 million people worldwide continues, with 1.8 million people newly infected each year. Highly active antiretroviral therapy is efficient at reducing viral load and nearly one-half of the infected population is on treatment. One of the most successful approaches for the treatment of HIV infections is the use of inhibitors for human immunodeficiency virus type-1 reverse transcriptase (HIV-1 RT). At present, there are six nonnucleoside reverse transcriptase inhibitors (NNRTIs) approved for clinical use: nevirapine (NVP), delavirdine (DLV), efavirenz (EFV), etravirine (ETV), rilpivirine (RPV), and elsulfavirine. In this review, we will cover the development of different classes of NNRTIs over the last two decades. We will give an overview of traditional medicinal chemistry strategies for structural modification as bioisosterism principles, scaffold hopping, substitute decoration, and molecular hybridization. Furthermore, computer-aid design as virtual screening, de novo design and free-energy perturbation will be described in details.

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Reference:
Oxazolidine – Wikipedia,
Oxazolidine | C3H339NO – PubChem

 

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Highly regio- and stereocontrolled synthesis of beta-substituted alpha-tributylstannyl enamides

The regio- and stereocontrolled synthesis of beta-substituted alpha-stannyl enamides is reported starting from internal ynamides. The synthesis of new ynamides as well as bis-ynamides is also described. Finally first examples of successful cross-coupling to afford alpha/beta-disubstituted enamides are also reported.

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Reference:
Oxazolidine – Wikipedia,
Oxazolidine | C3H382NO – PubChem

 

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HETEROCYCLIC COMPOUND

The present invention provides a compound having a superior JAK inhibitory action, which is useful as an agent for the prophylaxis or treatment of autoimmune diseases (rheumatoid arthritis, psoriasis, inflammatory bowel disease, Sjogren’s syndrome, Behcet’s disease, multiple sclerosis, systemic lupus erythematosus, etc.), cancer (leukemia, uterine leiomyosarcoma, prostate cancer, multiple myeloma, cachexia, myelofibrosis, etc.) and the like, or a salt thereof. The present invention relates to a compound represented by the formula wherein each symbol is as defined in the specification, or a salt thereof.

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Reference£º
Oxazolidine – Wikipedia,
Oxazolidine | C3H178NO – PubChem

 

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Synthetic Route of 497-25-6, Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In some cases, the catalyzed mechanism may include additional steps.In a article, 497-25-6, molcular formula is C3H5NO2, introducing its new discovery.

Copper-catalyzed coupling of amides and carbamates with vinyl halides

(Matrix presented) A general and efficient copper-catalyzed method for the amidation of vinyl bromides and iodides has been developed. This protocol uses a combination of 5 mol % copper iodide and 20 mol % N,N?-dimethyl ethylenediamine. Substrates bearing ester, silyl ether, and amino groups were successfully coupled under the reaction conditions. The double bond geometry of the vinyl halides was retained under the reaction conditions.

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Reference£º
Oxazolidine – Wikipedia,
Oxazolidine | C3H664NO – PubChem

 

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Design, synthesis and antitumor study of a series of N-Cyclic sulfamoylaminoethyl substituted 1,2,5-oxadiazol-3-amines as new indoleamine 2, 3-dioxygenase 1 (IDO1) inhibitors

Indoleamine 2, 3-dioxygenase 1 (IDO1) plays a key role in tryptophan catabolism which is an important mechanism in immune tolerance. The small molecule epacadostat is the most advanced IDO1 inhibitor, but its phase III trials as a single agent or in combinations with PD-1 antibody failed to show appreciable objective responses. To gain more insight on the antitumor efficacy of IDO1 inhibitors, we have designed a series of analogues of epacadostat by incorporating a cyclic aminosulfonamide moiety as the sidechain capping functionality. Compound 5a was found to display significant potency against recombinant hIDO1 and hIDO1 expressed HEK293 cancer cells. This compound has improved physico-chemical properties, acceptable PK parameters as well as optimal cardiac safety. Similar to epacadostat, 5a is ineffective as single agent in the CT-26 syngeneic xenograft model, however, the combination of 5a with PD-1 antibody showed both elevated tumor growth inhibition and prolonged median life span.

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Reference£º
Oxazolidine – Wikipedia,
Oxazolidine | C3H429NO – PubChem

 

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Processes for the production of heterocyclic compounds

A ketonic heterocyclic compound having at least two heteroatoms in the ring is prepared by reacting a difunctional compound having the general formula STR1 in which R1, R2, R3 and R4 are members of the group consisting of aliphatic, aromatic, cycloaliphatic and heterocyclic hydrocarbons which may contain functional groups selected from –OH, –OR5, –COOH, –COOR5, –CN, –Cl, –Br, –I, –F, and –CO–R5, wherein R5 is an aliphatic, aromatic, cycloaliphatic or heterocyclic hydrocarbon; X is oxygen or sulphur; Y is sulphur or nitrogen; n is an integer ranging from 1 to 3, or zero; R6 is a hydrogen or a hydrocarbon radical included in the above definition of R1 R2 R3 and R4 ; and m is the valence of Y, with carbon monoxide and oxygen in the presence of a catalyst selected from selenium, selenium compounds and complexes of copper, in the temperature range of from room temperature to 80 C and in the pressure range of from 1 to 10 atmospheres.

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Reference£º
Oxazolidine – Wikipedia,
Oxazolidine | C3H146NO – PubChem

 

A new application about Oxazolidin-2-one

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Electric Literature of 497-25-6, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.497-25-6, Name is Oxazolidin-2-one, molecular formula is C3H5NO2. In a Article£¬once mentioned of 497-25-6

Gold(I)-catalyzed intramolecular tandem addition/Friedel – Crafts reactions between acyclic enamides and 1-arylalkynes

Electron-deficient acyclic enamine derivatives react with electron-rich 1-arylalkynes using cationic gold(I) species as catalysts in an intramolecular process to form annulated 1-amido-substituted indene derivatives as the major products. Yields for this process range between 21% and 98%. In some cases, a two-step process that includes a subsequent alkene isomerization is needed.

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Reference£º
Oxazolidine – Wikipedia,
Oxazolidine | C3H705NO – PubChem

 

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Process for the manufacture of alkyl compounds

Process for the manufacture of a compound of formula I wherein R1 is H, acyl, alkyl or carbamoyl, R2 is a linear alkyl or alkenyl group, preferably a linear alkyl group comprising from 6 to 20 carbon atoms and n is 0, 1, 2, or 3, which comprises reacting a compound of formula II wherein R1 and n are as above and X is a leaving group with a carbanionic reagent of formula II ???????? M-R2 wherein R2 is as above and M denotes a metal or a metal containing group.

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Reference£º
Oxazolidine – Wikipedia,
Oxazolidine | C3H205NO – PubChem

 

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Recent progress in the discovery and development of DNA gyrase B inhibitors

New antibacterials that modulate less explored targets are needed to fight the emerging bacterial resistance. DNA gyrase and topoisomerase IV are attractive targets in this search. These are both type II topoisomerases that can cleave both DNA strands, and can thus alter DNA topology during replication or similar processes. Currently, there are no ATP-competitive inhibitors of these two enzymes on the market, as the only aminocoumarin representative, novobiocin, was withdrawn due to safety concerns. The search for novel ATP-competitive inhibitors is a focus of ongoing industrial and academical research. This review summarizes the recent efforts in the design, synthesis and evaluation of GyrB/ParE inhibitors. The various approaches to achieve improved antibacterial activities are described, with particular reference to Gram-negative bacteria.

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Reference£º
Oxazolidine – Wikipedia,
Oxazolidine | C3H335NO – PubChem