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SPIRO COMPOUNDS AND PHARMACEUTICAL USE THEREOF

The Spiro compound represented by the following general formula [Ia], its pharmaceutically acceptable salt or a solvate thereof

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Oxazolidine | C3H1678NO – PubChem

 

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, 102029-44-7, name is (R)-4-Benzyl-2-oxazolidinone, introducing its new discovery. Computed Properties of C10H11NO2

Enantioselective multicomponent synthesis of fused 6-5 bicyclic 2-butenolides by a cascade heterobicyclisation process

The successive coupling of an alkoxy(aryl/heteroaryl)carbene complex of chromium with either a ketone or an imide lithium enolate and then a 3-substituted (H, TMS, PhCH2, PhCH2CH2, Me) propargylic organomagnesium reagent has afforded novel hydroxy-substituted bicyclic [4.3.0]-gamma-alkylidene-2-butenolides with three modular points that has allowed the efficient introduction of molecular complexity, including a homopropargylic alcohol core. The selective formation of these five- or six-component heterobicyclisation products is the result of the regioselective integration of the Grignard reagent as a propargyl fragment followed by a cascade CO/alkyne/CO insertion, ketene trapping and elimination sequence. By using lithium enolates of chiral N-acetyl-2-oxazolidinones and the corresponding propargylic organocerium reagents, both enantiomers of these bicyclic heterocycles were efficiently prepared with very high enantiomeric purity. Architecturally, these fused bicyclic butenolides are characterised by a highly unsaturated and oxygenated core and they exhibit strong blue fluorescence in solution.

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In heterogeneous catalysis, the catalyst is in a different phase from the reactants. Recommanded Product: (R)-4-Benzyl-2-oxazolidinone, At least one of the reactants interacts with the solid surface in a physical process called adsorption in such a way. 102029-44-7, name is (R)-4-Benzyl-2-oxazolidinone. In an article£¬Which mentioned a new discovery about 102029-44-7

CERTAIN MACROCYCLIC LACTAM DERIVATIVES

The invention relates to macrocyclic lactam derivatives of formula I STR1 wherein R is hydrogen or acyl; m is an integer from 4 to 9 inclusive; n is 1 or 2; p is zero, 1 or 2; X is–CONH–or–NHCO–; Y is S, O or CH 2 ; R 1 is–COOH; or R 1 is STR2 in which R 2 is hydrogen, lower alkyl, aryl-lower alkyl, amino-lower alkyl, hydroxy-lower alkyl, acyloxy-lower alkyl, lower alkoxy-lower alkyl, mercapto-lower alkyl, lower alkyl-(thio, sulfinyl or sulfonyl)-lower alkyl, or carboxy-lower alkyl, R 3 is hydrogen or lower alkyl, and q is zero or an integer from 1 to 5 inclusive; or R 1 is STR3 in which R 4 is hydrogen, lower alkyl, lower alkoxy, hydroxy or acyloxy, and r is 1 or 2; or R 1 is STR4 in which s is 1 or 2; or R 1 is STR5 in which R 5 and R 6 independently represent hydrogen, lower alkyl, C 5-or C 6-cycloalkyl, (hydroxy-, acyloxy or lower alkoxy-) lower alkyl, carbocyclic or heterocyclic monocyclic aryl, or (hydroxy-, acyloxy-or alkoxy-) lower alkyloxy-lower alkyl; or R 5 and R 6 together with the nitrogen to which they are attached represent pyrrolidino, piperidino, morpholino, piperazino or N-alkylpiperazino; and macrocyclic sulfur and oxygen containing lactam ring isomers in which a CH 2 group of (CH 2) m in formula I is replaced by O or S, and Y represents CH 2 ; and pharmaceutically acceptable prodrug esters of any above said compound with a free carboxyl group; and pharmaceutically acceptable salts of any said compounds with a free acid or basic salt forming group; pharmaceutical compositions comprising said compounds; methods for the preparation of said compounds and for the preparation of intermediates; and methods of treating disorders in mammals which are responsive to the inhibition of neutral endopeptidases by administration of said compounds to mammals in need of such treatment.

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NITROGEN-CONTAINING HETEROCYCLIC COMPOUND AND USE THEREOF

The present invention relates to a compound represented by the formulawherein ring A is a nitrogen-containing heterocycle optionally further having substituent(s), ring B is an aromatic ring optionally having substituent(s), ring C is a cyclic group optionally having substituent(s), R1 is a hydrogen atom, a hydrocarbon group optionally having substituent(s), an acyl group, a heterocyclic group optionally having substituent(s) or an amino group optionally having substituent(s), R2 is an optionally halogenated C1-6 alkyl group, m and n are each an integer of 0 to 5, m+n is an integer of 2 to 5, and is a single bond or a double bond, or a salt thereof and the like. Since the compound has a superior tachykinin receptor antagonistic action, and is useful as an agent for the prophylaxis or treatment of various diseases such as lower urinary tract diseases, gastrointestinal diseases, central nervous system diseases and the like.

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Application of 102029-44-7, Chemistry is the science of change. But why do chemical reactions take place? Why do chemicals react with each other? The answer is in thermodynamics and kinetics.In a document type is Article, and a compound is mentioned, 102029-44-7, (R)-4-Benzyl-2-oxazolidinone, introducing its new discovery.

(S)-N-(5-Chlorothiophene-2-sulfonyl)-beta,beta-diethylalaninol a Notch-1-sparing gamma-secretase inhibitor

Accumulation of beta-amyloid (Abeta), produced by the proteolytic cleavage of amyloid precursor protein (APP) by beta- and gamma-secretase, is widely believed to be associated with Alzheimer’s disease (AD). Research around the high-throughput screening hit (S)-4-chlorophenylsulfonyl isoleucinol led to the identification of the Notch-1-sparing (9.5-fold) gamma-secretase inhibitor (S)-N-(5-chlorothiophene-2-sulfonyl)-beta,beta-diethylalaninol 7.b.2 (Abeta 40/42 EC50 = 28 nM), which is efficacious in reduction of Abeta production in vivo.

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The stereoselective total synthesis of (-)-dihydrotetrabenazine

A highly stereoselective synthesis of (-)-dihydrotetrabenazine has been accomplished using (R)-tert-butanesulfinamide as a chiral source. The synthesis involves the allylation of chiral N-sulfinyl imine followed by ring closure of the resulting secondary amide with a tethered halide and the Evans-Aldol reaction as key steps.

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Total synthesis of (-)-mucocin

An enantioselective total synthesis of (-)-mucocin has been completed. A combination of asymmetric glycolate aldol additions and ring closing metathesis reactions were exploited to construct the C18-C34 and C7-C17 fragments. A selective cross-metathesis reaction was employed as the key step to couple two complex fragments.

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Reference of 102029-44-7, 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, 102029-44-7, molcular formula is C10H11NO2, introducing its new discovery.

Process for the preparation of kinase inhibitors and intermediates thereof

Described are processes for the synthesis of certain compounds, useful for treating diseases, e.g. eye disease, such as glaucoma and ocular hypertension, in a subject.

The proportionality constant is the rate constant for the particular unimolecular reaction. the reaction rate is directly proportional to the concentration of the reactant. I hope my blog about 102029-44-7 is helpful to your research. Reference of 102029-44-7

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Oxazolidine – Wikipedia,
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Chemistry is traditionally divided into organic and inorganic chemistry. Application In Synthesis of (R)-4-Benzyl-2-oxazolidinone, The former is the study of compounds containing at least one carbon-hydrogen bonds.In a patent£¬Which mentioned a new discovery about 102029-44-7

(S)-beta3-homolysine- and (S)-beta3-homoserine-containing beta-peptides: CD spectra in aqueous solution

For further structural studies and for physiological investigations of beta-peptides, it is necessary to have H2O-soluble derivatives. Thus, we have prepared beta-hexa-, beta-hepta-, and beta-nonapeptides (1-6) with two, three, and seven side chains of lysine and serine. To detect possible pi-pi interactions, we also included the beta-amino acid beta2-HHop, resulting from homologation of so-called homophenylalanine (Hop) (5 and 6). The Fmoc-beta2- and beta3-amino-acid derivatives (11-14 and 19), and the corresponding beta- peptides were prepared by methods previously described (solid-phase peptide coupling; HPLC-pure samples, Fig. 1). Circular-dichroism spectra (Fig. 2) indicate the presence of less pronounced secondary structures (especially of the lysine analogues with multiple positive charge) in H2O as compared to MeOH. The beta3-heptapeptide (3) with two serine side chains is well soluble in H2O and exhibits the CD pattern typical of the 31-helical structure.

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Asymmetric Total Synthesis and Biological Evaluation of Proapoptotic Natural Myrcene-Derived Cyclohexenyl Chalcones

Based on a bioinspired asymmetric Diels?Alder cycloaddition using a chiral Evans oxazolidinone, the first total synthesis of both enantiomers of two myrcene-derived cyclohexenyl chalcones, fislatifolione and fislatifolic acid, has been carried out. This strategy was also applied to the total synthesis of nicolaiodesin C. These natural products, as well as their synthetic intermediates, were evaluated by in-vitro affinity displacement assays, based on the modulation of Bcl-xL/Bak, Mcl-1/Bid, and Bcl-2-Bim interactions. This study showed that (+)-fislatifolic acid acts as a dual Bcl-xL/Mcl-1 inhibitor with micromolar activity, and that a Weinreb amide intermediate acts as an excellent Mcl-1/Bcl-2 dual inhibitor at the submicromolar level.

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