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RADIOLABELED COMPOUNDS AND THEIR USE AS RADIOTRACERS FOR QUANTITATIVE IMAGING OF PHOSPHODIESTERASE (PDE10A) IN MAMMALS

The present invention provides radiolabeled compounds useful as radiotracers for quantitative imaging of PDE10A in mammals. The compound of the present invention is represented by the formula (I): wherein each symbols are as defined in the specification.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H232NO – PubChem

 

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FUSED BICYCLIC PYRAZOLE DERIVATIVES AS KINASE INHIBITORS

A series of substituted pyrazolo[1,5-alpha][1,3,5]triazine and pyrazolo[1,5-alpha]-pyrimidine derivatives, being selective inhibitors of PI3 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, ontological, nociceptive or ophthalmic conditions. Formula (I)

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Oxazolidine – Wikipedia,
Oxazolidine | C3H10NO – PubChem

 

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OXAZOLIDINONE COMPOUNDS AND THEIR USES IN PHARMACEUTICALS

The invention relates to the field of blood coagulation, more specifically it relates to novel oxazolidinone compounds or a pharmaceutically acceptable salt thereof, and their uses in the manufacture of medicaments for treating thromboembolic disorders or inhibiting factor Xa.

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Reference£º
Oxazolidine – Wikipedia,
Oxazolidine | C3H263NO – PubChem

 

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Direct Catalytic Desaturation of Lactams Enabled by Soft Enolization

A direct catalytic method is described for the alpha,beta-desaturation of N-protected lactams to their conjugated unsaturated counterparts under mildly acidic conditions. The reaction is consistently operated at room temperature and tolerates a wide range of functional groups, showing reactivity complementary to that of prior desaturation methods. Lactams with various ring sizes and substituents at different positions all reacted smoothly. The synthetic utility of this method is demonstrated in a concise synthesis of Rolipram. In addition, linear amides also prove to be competent substrates, and the phthaloyl-protected product serves as a convenient precursor to access various conjugated carboxylic acid derivatives. Strong bases are avoided in this desaturation approach, and the key is to merge soft enolization with a Pd-catalyzed oxidation process.

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Reference£º
Oxazolidine – Wikipedia,
Oxazolidine | C3H424NO – PubChem

 

Can You Really Do Chemisty Experiments About Methyl (R)-N-Boc-2,2-dimethyloxazolidine-4-carboxylate

We¡¯ll also look at important developments in the pharmaceutical industry because understanding organic chemistry is important in understanding health, medicine, the role of 95715-86-9, and how the biochemistry of the body works.Computed Properties of C12H21NO5

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Synthesis of N-(tert-butoxycarbonyl)-N,O-isopropylidene serinal from serine methyl ester by a reduction-oxidation sequence

The title aldehyde is prepared by LiAlH4 reduction of the corresponding serine derived methyl ester to the alcohol and Swern oxidation of the latter. The aldehyde is obtained in 94 % yield and 96-98 % enantiomeric purity. This method avoids some problems encountered in the synthesis of the same aldehyde by direct controlled DIBAL reduction of the ester.

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Reference£º
Oxazolidine – Wikipedia,
Oxazolidine | C3H2508NO – PubChem

 

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Diastereoselective [2,3]-Sigmatropic Rearrangement of N-Allyl Ammonium Ylides

A rapid and diastereoselective method was developed for the [2,3]-sigmatropic rearrangement of N-Allyl ammonium ylides, affording products in up to 95% isolated yields and up to 97:3 dr; most of the desired products were formed within 1 minute. For the asymmetric reaction, a chiral auxiliary was introduced to the starting compound, affording the rearrangement product with high diastereoselectivities.

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Reference£º
Oxazolidine – Wikipedia,
Oxazolidine | C3H850NO – PubChem

 

Extracurricular laboratory:new discovery of Methyl (R)-N-Boc-2,2-dimethyloxazolidine-4-carboxylate

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Design and optimization of new phosphine oxazoline ligands via high- throughput catalyst screening

This paper uses the phosphine oxazoline ligands 1 and an allylation transformation (reaction 1) to illustrate the value of divergent ligand syntheses and high-throughput screening in catalyst discovery and optimization. Thus, a diverse set of ligands 1 (Table 1) was prepared via a divergent synthesis involving the pivotal intermediate, phosphine-substituted amino alcohol 7 (Scheme 1). Single-crystal X-my crystallographic data was obtained for a nickel complex 8 (Figure 3) of the phenyl-substituted ligand 1i. This analysis illustrated some structural features of the ligand systems 1 that may be conducive to asymmetric catalysis. High-throughput screens were then used to correlate the ligand 1 R-substituents with asymmetric induction in the allylation reaction 1, and it emerged that the pseudo-spherical adamantyl substituent was superior to other R-substituents. Other parameters in the catalyst systems were also varied, sometimes in ‘two-dimensional’ screens. No pronounced solvent effects were identified. Abstraction of chloride was shown to be detrimental, whereas addition of chloride provided no advantages. One of the most critical of all the variables probed was, rather surprisingly, the effect of ligand-to-metal ratio; enantioselectivities dropped sharply and eventually reversed when this ratio was increased above 1:1. These observations were rationalized in terms of a chelated complex A and a nonchelated one B (Scheme 3). The implications of these results for high-throughput screening of catalyst systems in general, and for ligands 1 in particular, are discussed.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H2551NO – PubChem

 

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Hexahydro-trans- and tetrahydropyridoindole neuroleptic agents

Derivatives of 2,3,4,5-tetrahydro-1H-pyrido[4,3-b]-indole and of (+)enantiomeric, mixtures of (+) and (-)enantiomeric or (¡À)racemic 2,3,4,4a,5,9b-hexahydro-4a,9b-trans-1H-pyrido[4,3-b]indole, substituted at the 5-position with an aryl group and at the 2-position with a carbonylaminoalkyl group or an aminoalkyl group, are neuroleptic agents useful in the treatment of certain psychoses and neuroses.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H247NO – PubChem

 

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Synthetic studies on lytophilippine A: Synthesis of the proposed structure

Chemical equations presented. Synthesis of the proposed structure of lytophilippine A was accomplished employing SmI2-mediated 5-exo cyclization of an aldehydo beta-alkoxyvinyl sulfoxide and ring-closing metathesis reaction.

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Oxazolidine – Wikipedia,
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ASPARTYL PROTEASE INHIBITORS

A compound of formula (I): N-oxides, addition salts, quaternary amines metal complexes stereochemically isomeric forms and metabolites thereof, wherein A is CR1 or N; D is H, C1-C6alkyl, C2-C6alkenyl, C2-C6alkynyl or Q is C2-C6alkenyl, C2-Cealkynyl, aryl or heterocyclyl; W is H, Ci-Cealkyl, C2-C6alkenyl, haloC1-C3alkyl, hydroxyC1-C3alkyl, C3-C6Cy cloalkyl, aryl or heterocyclyl; one of X’ and X” is H or CH3, the other is C1-C3alkyl, F, OH, NRaRb, CF3 or N3; or X’ and X” are both F; Y is a bond, CH2, NRa, O, CH2CH2, CH2NRa, CH2O or S(=O)r; Z is O, S(=O)r or NRa; the other variables are as defined in the specification. The compounds of the invention are inhibitors of BACE and are among other things useful for the treatment and/or prevention of conditions associated with BACE activity such as Alzheimer’s disease.

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Reference£º
Oxazolidine – Wikipedia,
Oxazolidine | C3H160NO – PubChem