A (2R,4S)-trans-disubstituted pyrrolidine ring system was constructed by employing iodine-mediated oxidative cyclization of (1R)-N-[1-(4-bromophenyl)-3-butenyl]acetamide 3 as a key step. The resulting diastereomeric mixture of (2R)-2-aryl-4-acetoxypyrrolidine 4 was stereoselectively converted to the side-chain of a novel ultrabroad-spectrum carbapenem 1, via (2R,4R)-2-aryl-4-hydroxypyrrolidine 7.

BACKGROUND Dialkyl 1,4-dihydro-2,6-dimethylpyridine-3,5-dicarboxylates (1,4-DHP) have now been recognized as vital drugs. Some of these derivatives such as amlodipine, felodipine, isradipine, etc. have been commercialized. In view of wide range of biological properties associated with 1,4-DHP and owing to the biological importance of the oxidation step of 1,4-DHP, we carried out the synthesis a...

The tankyrases are members of the PARP superfamily; they poly(ADP-ribosyl)ate their target proteins using NAD(+) as a source of electrophilic ADP-ribosyl units. The three principal protein substrates of the tankyrases (TRF1, NuMA and axin) are involved in replication of cancer cells; thus inhibitors of the tankyrases may have anticancer activity. Using structure-based drug design and by analogy...

Chemical modification is an important technique to modulate the chemical and optical properties of graphene quantum dots (GQDs). In this paper, we report a versatile diazonium chemistry method to graft aryl groups including phenyl, 4-carboxyphenyl, 4-sulfophenyl and 5-sulfonaphthyl to GQDs via Gomberg-Bachmann reaction. The aryl-modified GQDs are nanocrystals with lateral dimensions in the rang...

Aryl-cobalamins are a new class of organometallic structural mimics vitamin B12 designed as potential ‘antivitamins B12’. Here, the first cationic aryl-cobinamides described, which were synthesized using newly developed diaryl-iodonium method. The obtained pairs coordination isomers, stereo-structure was unambiguously assigned based on homo- and heteronuclear NMR spectra. availability isomers w...

A series of new 2-arylimino-3-aryl-5-[5?-(3,4-dichlorophenyl)-2?-furylidene]-4-thiazolidinones (3a-l) have been synthesised by the condensation of 5-(3,4-dichlorophenyl)-2-furaldehyde 1 with 2-arylimino-3-aryl-5H-4-thiazolidinones 2 in glacial acetic acid. The physical and spectral data of the synthesised compounds are determined. The synthesised compounds have been screened for their in vitro ...

the aryl-(z)-n-[2-amino-1,2-dicyanovinyl]formamidine 2 cyclize in solvent-free conditions and in the presence of a base to give a 5-amino-1-aryl-4-cyanoimidazoles 3. silica sulfuric acid as an efficient and reusable heterogeneous catalyst has been used for the preparation of amidines 2 from formimidate 1 through reaction with aromatic amines at room temperature and in good to excellent yields. ...

Z. Naturforsch. 56 b, 1172-1177 (2001); received July 13, 2001 Aryl Formates, Formylation, Hydroxyarenes Aryl formates 4a-u, 6 , 8 , 10, 12, 14, 16, 18, 20, 22, 24, 26 are prepared by formylation of hydroxyarenes 3a-u, 5, 7, 9, 11, 13, 15, 17, 19, 21, 23, 25 with /V,Af-diformylacetamide (1) or triformamide (2), respectively, in fairly good yields. The reactions can be catalyzed by sodium diform...