83791-43-9

Upstream product

• 67-56-1 methanol 
• 1195-20-6 (5R,4S)-5-methyl-2-oxazolidinone-4-carboxylic acid 
• 32315-10-9 bis(trichloromethyl) carbonate 
• 39994-75-7 L-threonine methyl ester hydrochloride 
• 72-19-5 L-threonine 
• 332-25-2 4-(trifluoromethoxy)benzonitrile 
• 83791-38-2 5-methyl-2-oxo-2,3-dihydro-1,3-oxazole-4-carboxylic acid methyl ester 
• 3373-59-9 allo-Thr-OMe 
• 80465-30-1 N-carboxy 2-amino-2-butenoic acid anhydride 
• 83791-33-7 4-(1-Bromo-ethyl)-4-methoxy-oxazolidine-2,5-dione 
• 163254-35-1 methyl 3-((tert-butoxycarbonyl)amino)butanoate 

Downstream Products

• 60538-19-4 N-(tert-butoxycarbonyl)-l-threonine methyl ester 
• 128062-14-6 C₅H₈N₂O₃ 

Relevant academic research and scientific papers

Visible-Light-Mediated Liberation and In Situ Conversion of Fluorophosgene

The first example for the photocatalytic generation of a highly electrophilic intermediate that is not based on radical reactivity is reported. The single-electron reduction of bench-stable and commercially available 4-(trifluoromethoxy)benzonitrile by an organic photosensitizer leads to its fragmentation into fluorophosgene and benzonitrile. The in situ generated fluorophosgene was used for the preparation of carbonates, carbamates, and urea derivatives in moderate to excellent yields via an intramolecular cyclization reaction. Transient spectroscopic investigations suggest the formation of a catalyst charge-transfer complex-dimer as the catalytic active species. Fluorophosgene as a highly reactive intermediate, was indirectly detected via its next downstream carbonyl fluoride intermediate by NMR. Furthermore, detailed NMR analyses provided a comprehensive reaction mechanism including a water dependent off-cycle equilibrium.

INHIBITOR CONTAINING TRICYCLIC DERIVATIVE, PREPARATION METHOD THEREFOR, AND APPLICATION THEREOF

An inhibitor containing a tricyclic derivative, a preparation method therefor and a pharmaceutical composition comprising the inhibitor, as well as a use thereof as a phosphoinositide 3 kinase (PI3K) inhibitor in the treatment of cancer and diseases or conditions mediated by or dependent on PI3K imbalance.

Crystal form containing triple-fused-ring derivative free alkali and pharmaceutical composition thereof

The invention relates to a crystal form containing triple-fused-ring derivative free alkali and a pharmaceutical composition thereof. The invention specifically relates to a crystal form of a compound free alkali with a general formula (I), a preparation method, a pharmaceutical composition containing a therapeutically effective amount of the crystal form, and an application of the crystal form in preparation of drugs for treating PI3K-mediated related diseases.

PYRAZOLYL DERIVATIVES AS SYK INHIBITORS

The present invention provides novel pyrazole derivatives of formula I which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD, rheumatoid arthritis, and cancer.

Pd-catalyzed carboamination of oxazolidin-2-ones: A stereoselective route to trans -2,5-disubstituted pyrrolidines

Palladium-catalyzed carboamination reactions between aryl bromides and 4-(but-3-enyl)-substituted oxazolidin-2-ones are described. These transformations afford bicyclic oxazolidin-2-one derivatives that can be converted to trans-2,5-disubstituted pyrrolid

Stereoselective syntheses of (E)-α,β-didehydroamino acid and peptide containing its residue utilizing oxazolidinone derivative

Reaction of methyl N-Boc-N-phenoxycarbonylglycinate with various aldehydes afforded the corresponding cis-4,5-oxazolidinone derivatives, which were effectively converted to (E)-α,β-didehydroamino acids by means of a base. Furthermore, N-deprotection of the oxazolidinone derivatives and subsequent coupling reaction with Boc-amino acid furnished the corresponding dipeptides, which were transformed to dipeptide containing α,α- didehydroamino acid with high E selectivity.

Rational design of an L-histidine-derived minimal artificial acylase for the kinetic resolution of racemic alcohols

This communication describes the rational design of an l-histidine-derived minimal artificial acylase. Our new artificial acylase, tert-butyldiphenylsilyl ether of N-(2,4,6-triisopropylbenzenesulfonyl)-π(Me)-l-histidinol, is a simple and small molecule (m

Novel synthesis of 4-carboxymethyl 5-alkyl/aryl oxazolidin-2-ones by rearrangement of 2-carboxymethyl 3-alkyl/aryl N-tert-butoxycarbonyl aziridines

(matrix presented) A two-step approach for the diastereoselective synthesis of 4-carboxymethyl 5-alkyl/aryl oxazolidin-2-ones is described, which proceeds via the intermediate formation of 2-carboxymethyl 3-alkyl/aryl N-tert-butoxycarbonyl (N-Boc) aziridines. By reaction of N-Boc β-amino methyl esters with LiHMDS and iodine, trans 2,3-disubstituted N-Boc aziridines are obtained with high stereoselectivities and yields. The final rearrangement to oxazolidin-2-ones is achieved by treatment with a catalytic amount of a Lewis acid and proceeds with high yield and complete regio- and stereoselectivity.

Enhanced enantiocontrol in catalytic metal carbene transformations with dirhodium(II) tetrakis, Rh2(4S-MEOX)4

The synthesis, spectral characteristics, and X-ray structures for dirhodium(II) tetrakis, Rh2(4S-MEOX)4, and the related dirhodium(II) tetrakis, Rh2(4S-THREOX)4, are reported.Comparison is made between these 2-oxooxazolidin-ligated dirhodium(II) catalysts for metal carbene transformations and those with comparable 2-oxopyrrolidine ligands, especially dirhodium(II) tetrakis, Rh2(5S-MEPY)4.Structure-selectivity comparisons reveal that Rh2(4S-MEOX)4 provides higher enantiocontrol and, in some cases, higher diastereocontrol than Rh2(5S-MEPY)4 in intramolecular carbon-hydrogen insertion reactions of sterically demanding diazoacetates and diazoacetamides and is the catalyst of choice for highly enantioselective diazodecomposition of adamantyl diazoacetates and N-(tert)butyldiazoacetamides.The structurally analogous Rh2(4S-THREOX)4 is nearly identical with Rh2(4S-MEOX)4 in its overall effect on selectivity.The net advantage of Rh2(4S-MEOX)4 lies in its wider openness for metal carbene transformations.