Insulin-like growth factor 1 (IGF1) actions are essential for somatic growth and tissue repair. IGF1 gene regulation is controlled by many inputs, with growth hormone playing a major role. In most mammals, the 6-exon IGF1/Igf1 gene produces multiple transcripts via independent activity of its pr...

The thermal degradation of oligomers of 9-(2,3-epoxypropyl)carbazole synthesized by the action of anionic (KOH) and cationic (BF3Et2O) catalysts has been investigated using the techniques of thermogravimetry, differential thermal analysis (DTA) and gel permeation chromatography (GPC). Kinetic pa...

The title pentasaccharide was synthesized via a 2 + 3 strategy. The disaccharide donor, 3-O-acetyl-2-O-benzoyl-4,6-O-benzylidene-β-d-glucopyranosyl-(1→3)-2-O-benzoyl-4,6-O-benzylidene-α-d-glucopyranosyl trichloroacetimidate (8), was obtained by selective coupling of allyl 2-O-benzoyl-4,6-O-be...

Photocopolymerization of 9-(2,3-epoxypropyl)carbazole (EPC) with tetrahydrofuran (THF) initiated with di-(tert-butyl phenyl)iodonium tetrafluoroborate has been studied. The influence of temperature on the rate of the comonomer consumption has been investigated. The dependence of THF and EPC conv...

Comparative investigation of photoconductivity sensitisation of poly-N-(2,3-epoxypropyl)carbazole by electron acceptors of the fluorene (1–2) and tetracyanoquinodimethane (3–5) series shows that fluorene acceptors are more efficient giving the electrophotographic films with higher integral pho...

The novel purine and pyrimidine nucleoside analogues possessing a 2,3-epoxypropyl (2a–2c and 8a–8c), 2,3-epoxypropyl ether (3), or 3-amino-2-hydroxypropyl (4a–6c and 9a–9c) moiety bonded at either N-9 of the C-6 substituted purine ring or N-1 and N-3 of the pyrimidine ring, were prepared and...

A catalytic enantioselective desymmetrization of meso-N-(heteroarenesulfonyl)aziridines with TMSN3 using chiral Lewis acids afforded products with high enantioselectivity. As proof of the utility of this procedure, the precursor of selective κ-opioid agonist (1S,2S)-(−)-U-50,488 was synthesized.

Publisher SummaryThis chapter discusses the chemistry of carbohydrate aziridines, with emphasis being placed on surveying preparative methods and ring-opening reactions. Carbohydrate aziridines or epimines are derivatives in which an aziridine ring is fused to a pyranose or furanose ring or to a...

Lithiation of 1-methylaziridine borane, 1-(tert-butyldimethylsiloxyethyl)aziridine borane, or 1-(tert-butyldimethylsiloxyethyl)-2-methylaziridine borane occurs syn to the boron substituent, while lithiation of 1-(tert-butyldimethylsiloxyethyl)-2-trimethylstannylaziridine borane occurs anti to bo...

This review covers the literature on fused-ring aziridines and azirines from late 1995 through 2006. The review considers the two general types of fused-ring aziridines. The two structural classes of fused-ring aziridines are: (1) fused-ring aziridines with the aziridine nitrogen at the bridgehe...

A new class of quinazoline-based enantiomerically pure aziridine diols 4a–d were prepared from the aziridination of mesityl oxide 3 with in situ generated 3-acetoxyaminoquinazolinone (S)-2b followed by NaBH4 reduction. Aziridine diols 4a–d were purified by means of column chromatography on sil...

Desymmetrization of meso-aziridines with aromatic thiols was realized by using α-amino acids-derived chiral quaternary phosphonium salts catalysts to provide chiral β-amino sulfides with high yields (up to 99%) and in moderate enantioselectivities (up to 70%).

A survey of the chemical literature published between 1995 and 2007 dealing with the chemical reactivity and synthesis of monocyclic aziridines and 2H-azirines is presented. The reactivity of monocyclic aziridines is discussed first, specifically including sections on nucleophilic ring-opening r...

A facile and effective synthesis of 6-aryluracil derivatives was accomplished by the direct C–H bond activation for arylation. A series of 6-aryl-1,3-dimethyluracils were synthesized from the reaction of 1,3-dimethyluracil with various phenyl iodides in DMF, in the presence of copper(I) bromide...

Herein we report, a series of new benzimidazolium chlorides as N-heterocyclic carbene (NHC) ligand and their corresponding palladium(II)-NHC complexes with the general formula [PdCl2(NHC)2] were synthesized. All new compounds were characterized by 1H NMR, 13C NMR, IR spectroscopy and elemental a...

Bifunctional DNA cross-linking agents are widely used as chemotherapeutic agents in clinics. The advance in the development of these agents as potential antitumor agents has generated various types of bis(hydroxymethyl)pyrrole analogs. In order to develop highly effective anticancer agents, it i...

The synthesis of 4-hydroxymethyl-2,4-methanoproline, a novel conformationally restricted amino acid, was performed in four steps. This close analogue of naturally occurring amino acids (i.e., proline, hydroxyproline, serine and threonine) was prepared in good overall yield through two intramolec...

A method of synthesis of 1,2-bis(3,4-dicyanophenoxymethyl)benzene from the 1,2-bis(hydroxymethyl)benzene and 4-nitrophthalodinitrile is developed. Its tetramerization with Zn(OAc)2·2H2O gives a binuclear zinc phthalocyanine of a new type, containing four o-phenylidene bridges. The use of microw...

The synthesis of 5-hydroxymethyl furfural (HMF) from cellulose via a two-step process was investigated. To optimize reaction conditions, the separate conversion of cellulose and glucose was first performed in tetrahydrofuran (THF) and N, N-dimethylformamide (DMF) via a one-step process using hos...

The synthesis and biological evaluation of 6,7-bis(hydroxymethyl)-1H,3H-pyrrolo[1,2-c]thiazoles as anticancer agents against MCF7 breast cancer cell lines is reported. The design of the new compounds has been guided considering (3R)-6,7-bis(hydroxymethyl)-5-methyl-3-phenyl-1H,3H-pyrrolo[1,2-c]th...