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Predictable and regioselective insertion of internal unsymmetrical alkynes in rhodium-catalyzed cycloadditions with alkenyl isocyanates

A regioselective, rhodium-catalyzed cycloaddition between a variety of internal, unsymmetrical alkynes is described. We document the impact of both steric and electronic properties of the alkyne on reaction course, efficiency, and enantioselectivity. The substituent that better stabilizes a positive charge or the larger group, all else being equal, inserts distal to the carbonyl moiety in a predictable and controllable fashion. The reaction scope is broad and the enantioselectivities are high, providing an “instruction manual” for substrate choice when utilizing this reaction as a synthetic tool.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H529NO – PubChem

 

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Poly(N-vinylimidazole) as an efficient and recyclable catalyst of the aza-Michael reaction in water

Poly(N-vinylimidazole) effectively catalyzed Michael addition of 1H-1,2,4-triazole, 3,5-dimethyl-1H-1,2,4-triazole, uracil, oxazolidin-2-one, and succinimide to but-3-en-2-one, cyclohex-2-en-1-one, methyl acrylate, and methyl vinyl sulfone in water at room temperature. The catalyst can readily be regenerated and repeatedly used at least five times without loss in activity, as shown in the reaction of 1H-1,2,4-triazole with but-3-en-2-one as an example.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H344NO – PubChem

 

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Pyridazinone compounds

The present invention provides a compound which has the effect of PDE inhibition, and which is useful as a medicament for preventing or treating schizophrenia or so on. A compound of formula (I0): wherein R1 represents a substituent, R2 represents a hydrogen atom, or a substituent, R3 represents a hydrogen atom, or a substituent, Ring A represents an aromatic ring which can be substituted, and Ring B represents a 5-membered heteroaromatic ring which can be substituted, or a salt thereof.

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Oxazolidine – Wikipedia,
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NOVEL NAPHTHYRIDINES AND ISOQUINOLINES AND THEIR USE AS CDK8/19 INHIBITORS

The present invention relates to naphthyridine and isoquinoline compounds, and pharmaceutically acceptable compositions thereof, useful as inhibitors of CDK8/19, and for the treatment of CDK8/19-related disorders.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H218NO – PubChem

 

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Efficient and convenient palladium-catalyzed amination of allylic alcohols with N-heterocycles

Atom economic: A commercially available palladium catalyst system is applied for an environmentally benign allylation of electron-deficient N-heterocycles using allylic alcohols (see scheme). The system is also applied for the N-allylation of biologically important uridine and thymidine derivatives. Copyright

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Oxazolidine – Wikipedia,
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TETRAZINE-BASED BIO-ORTHOGONAL COUPLING REAGENTS AND METHODS

Coupling reactions, suitable for use in organic or aqueous media, are performed by contacting a 1,2,4,5-tetrazine with a dienophile. The dienophile may be covalently bonded to a protein, and the coupling reaction may be performed in biological media such as those containing cells or cell lysates. The reactions may be performed in the presence of primary amines, thiols, acetylenes, azides, phosphines, and products of Staudinger and/or Sharpless-Huisgen reactions Novel 3-substituted cyclopropene compounds and trans-cyclooctenes are exemplary dienophiles for these reactions.

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Oxazolidine – Wikipedia,
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A copper-catalyzed carbonylative four-component reaction of ethene and aliphatic olefins

To have a balance between reactivity and selectivity has been a long-standing challenge in multicomponent reactions. In this communication, a carbonylative four-component reaction has been developed. With copper as the catalyst, using ethene including other aliphatic alkenes, alcohols and acetonitrile as the substrates under CO pressure, various desired products were produced in moderate to good yields. The obtained products can be applied in the synthesis of delta-valerolactams. Good functional group tolerance and reaction efficiency can be observed here.

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Oxazolidine – Wikipedia,
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Facile formation of N-acyl-oxazolidinone derivatives using acid fluorides

A mild method is presented for the formation of N-acylated oxazolidinones that employs acid fluorides and mild bases, such as iPr 2NEt and NEt3. Optimized reaction conditions for two types of substrates have been developed utilizing either the oxazolidinone itself or the corresponding in situ generated O-silyloxazolidinones resulting in the formation of the desired N-acylated products in high yields of up to 98%.

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Cobalt-mediated regio- and stereoselective assembly of dienamides by hydroaminative alkyne coupling of alpha,omega-diynes

In the presence of CpCo(C2H4)2, alpha,omega-diynes undergo hydroaminative coupling with amides to furnish new dienamides with control of regio- and stereochemistry. The Royal Society of Chemistry.

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Uncatalysed intermolecular aza-Michael reactions

The catalyst-free reactions of activated alkenes with primary and secondary amines were investigated leading to various mono- and di-hydroamination products, the latter being rare and original. These reactions were shown to depend first on the strength of the nucleophile. Temperature and steric hindrance of the reagents were the other key factors controlling the selectivity of these aza-Michael reactions. In spite of their poor nucleophilicities, some N-heterocyclic amines could react with different activated alkenes affording valuable intermediates. Such results tended to demonstrate the hydrogen-bonding interactions between activated alkenes and poly-nitrogen aromatic cycles may control these concerted or fully conjugate aza-Michael additions.

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Oxazolidine – Wikipedia,
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