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Ergoline derivatives and acid addition salts thereof

Novel ergoline derivatives and acid addition salts thereof are disclosed. These ergoline derivatives possess excellent anti-hypertensive activity, vasodilating activity, anti-ulcer activity, gastric secretion inhibitory activity, brain metabolism improving activity, anti-depressive activity and dopamine-like activity, and, therefore, are useful for prevention and treatment of various diseases such as hypertension, a wide variety of vein disorders, peptic ulcer, brain absormality, depression, Parkinson’s disease, high prolactin blood disease, etc.

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Oxazolidine – Wikipedia,
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ZrCl4-catalyzed aza-Michael addition of carbamates to enones: Synthesis of Cbz-protected beta-amino ketones

The reaction of alpha,beta-unsaturated ketones with benzyl carbamate and 2-oxazolidinone was effectively promoted by a catalytic amount of zirconium (IV) chloride to produce the corresponding beta-amino ketones.

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Short communication: Silica sulfuric acid: A versatile and reusable heterogeneous catalyst for the synthesis of N-ACYL carbamates and oxazolidinones under solvent-free conditions

Silica sulfuric acid catalyzes efficiently the reaction of carbamates and oxazolidinones with anhydrides under solvent-free conditions. All the reactions were done at room temperature and the N-acyl carbamates and oxazolidinones were obtained with high yields and purity via an easy work-up procedure. This method is attractive and is in a close agreement with green chemistry.

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Steric and electronic requirements of amide and ester groups in benzylidenemalonates

Stereoisomeric benzylidinemalonates have been synthesised. In the case of N-(2-ethoxycarbonyl-3-phenylpropenoyl)-2-oxazolidinone, both E- and Z-isomers could be obtained, but the Z-isomer isomerised (> 95%) to the E-isomer in the presence of catalytic amounts of Rh(I) complex catalysts. For ethyl tert-butylamidobenzalmalonate, the Z-isomer initially predominates under Knoevenagel conditions, but is very readily converted into the more stable E-isomer, which is here isolated stereoisomerically pure and is the only product of other synthetic routes. The configuration of benzylidinemalonates was established in two cases by X-ray crystallography, and the relative stability of the isomeric forms correctly simulated by MM2 calculations. In both the amide and oxazolidinone series, asymmetric hydrogenation catalysed by cationic Rh complexes gave a configurationally stable product cleanly but in low e.e..

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Chiral non-racemic bicyclic lactams. Auxiliary-based asymmetric reactions

The chiral non-racemic bicyclic lactam has proven to be an exceptionally versatile chiral template for the asymmetric construction of a variety of optically pure compounds. Those lactams derived from keto acids have been applied to the synthesis of a host of natural products and pharmacologically interesting heterocycles and carbocycles. A variety of mechanistic questions regarding facial stereo-control have been investigated using the chiral template as the key probe. However, further elucidation of the subtle mechanistic principles involved await further study.

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INDENYL DERIVATIVES AND USE THEREOF FOR THE TREATMENT OF NEUROLOGICAL DISORDERS

The present invention relates to novel indenyl derivatives having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of neurological and psychiatric disorders.

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Kinetics of N-bromination of 2-oxazolidinone

The kinetics of N-bromination of 2-oxazolidinone by transferor Br from sodium hypobromite, N-bromosuccinimide (NBS), or N-bromoacetamide (NBA) were determined spectrophotometrically, at pH between 4.6 and 12.45 (depending on the brominating agent). The reaction with hypobromite was of first order with respect to both the hypobromite and the substrate. The bromination of oxazolidinone with NBS (or NBA) has been found to be a reversible process of order one with respect to both NBA (or NBA) and oxazolidinone in the forward direction, and order one with respect to SI (or ACAM) and the resulting N-bromo-oxazolidinone in the other. The pH dependence of the reaction rate was in keeping with a mechanism in which all the brominating agents (HOBr, BrO -, NBS and NBA) react predominantly with the anion of the substrate. Bimolecular bromination rate constants increased in the order BrO- < NBA < NBS < HOBr. Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data. HPLC of Formula: C3H5NO2, If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 497-25-6, in my other articles.

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Switchable palladium-catalyst reaction of bromomethyl sulfoxides, CO, and N-nucleophiles: Aminocarbonylation at Csp3 versus oxidative carbonylation of amines

The palladium-catalyzed reaction of alpha-bromomethyl sulfoxides, carbon monoxide, and N-nucleophiles follows different reaction pathways according to the catalytic system and the reaction conditions. The Pd-xantphos catalyst affords high yields of alpha-sulfinyl amides by an aminocarbonylation process and is the first example of this type of transformation for a nonbenzylic sp3-hybridized carbon. On the other hand, the oxidative carbonylation of amines occurs with alpha-bromomethyl sulfoxides, carbon monoxide, and catalytic Pd(PPh3)4 under aerobic conditions, yielding ureas and oxalamides from either primary or secondary amines. The reaction with ambident nucleophiles such as amino alcohols was highly selective and took place exclusively at the amino group despite the presence of the alcohol functionality. In parallel to the reaction paths for simple amines, amino alcohols were converted into hydroxy sulfinyl amides when the reaction was catalyzed by Pd-xantphos, while Pd(PPh3)4 catalyst afforded cyclic carbamates. The alkoxycarbonylation reaction of bromomethyl sulfoxides with simple alcohols and CO leading to the corresponding sulfinyl esters is also described.

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Dialkylzinc mediated radical additions to chiral N-enoyloxazolidinones in the presence of benzaldehyde. Mechanistic investigation, structural characterization of the resulting gamma-lactones

Diethylzinc was used in the presence of oxygen to mediate radical additions to chiral N-enoyloxazolidinones derived from fumaric acid. The synthesis of sterically crowded trisubstituted gamma-lactones was achieved through a multicomponent reaction involving t-butyl iodide and benzaldehyde in addition to the above mentioned reagents. The domino process includes successively: iodine atom transfer, radical addition, homolytic substitution at zinc, aldol condensation, and lactonization. The diastereoselectivity of the reaction and the structural features of the resulting lactones were investigated. A tentative rationalization is discussed. Comparative experiments carried out with diisopropylzinc were performed.

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AZAINDOLES AS INHIBITORS OF HPK1

Azaindole compounds and their use as inhibitors of HPK1 are described. The compounds are useful in treating HPK1-dependent disorders and enhancing an immune response. Also described are methods of inhibiting HPK1, methods of treating HPK1- dependent disorders, methods for enhancing an immune response, and methods for preparing the azaindole compounds.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H118NO – PubChem