PurposeThere are currently no approved therapies for patients with metastatic pancreatic adenocarcinoma previously treated with gemcitabine. This Phase III trial evaluated the efficacy and safety of glufosfamide as compared with best supportive care (BSC) in this patient population.

Glufosfamide is a new, potential chemotherapeutic agent currently under investigation. Stability of glufosfamide was investigated in sodium phosphate buffers with different pH and temperature and in biological samples. Glufosfamide and isophosphamide mustard were quantified simultaneously using ...

The reaction of 2-[(diphenylphosphino)methyl]-6-methylpyridine (PN) with Os3(CO)12−n(MeCN)n [where n = 0 (1), 1 (2), 2 (3)] has been investigated. Os3(CO)12 reacts with PN in the presence of Me3NO to afford the clusters Os3(CO)11(κ1-PN) (4) and 1,2-Os3(CO)10(κ1-PN)2 (5). X-ray diffraction anal...

The enantioselective synthesis of (R)-(−)-actisonitrile 1 has been achieved via O-alkylation of (4R,αS)-4-hydroxymethyl-3-(α-methylbenzyl)oxazolidin-2-one (αS)-4 with 1-iodohexadecane in the presence of CsOH in DMF. Under these reaction conditions, the O-alkylation was much faster than the in...

In continuation of our research program for new antituberculosis drugs, we have designed, synthesized and evaluated antimycobacterial activity of new series of 1-[3-(4-benzotriazol-1/2-yl-3-fluoro-phenyl)-2-oxo-oxazolidin-5-ylmethyl]-3-substituted-thiourea derivatives against different Mycobacte...

Reduction of (4S,5S,6S)-4-hydroxymethyl-5-iodo-6-methyl-1,3-oxazin-2-one 2a and (4S,5S,6R)-4-hydroxymethyl-5-iodo-6-phenyl-1,3-oxazin-2-one 2b with tributyltin hydride in ethanol afforded 1,3-oxazin-2-one 3a and 1,3-oxazolidin-2-one 4b, respectively. Hydrolysis of 3a and 4b under basic condition...

Chiral symmetrical alk-2-yne-1,4-diols have been stereoselectively transformed into 5-alkyl-4-alkenyl-4-phenyl-1,3-oxazolidin-2-ones, which are precursors of quaternary α-amino β-hydroxy acids. The key step was the cyclization of the bis(tosylcarbamates) of 2-phenylalk-2-yne-1,4-diols, easily ...

The capacity of N-Boc-4-hydroxymethyl-oxazolidin-2-ones to undergo rapid O–O and N–O acyl transfer makes these serine derived chiral auxiliaries unsuitable for attachment to polymers.

Compounds structurally related to the known antimicrobial drug linezolid were selected in order to evaluate the influence of electron-withdrawing properties and altered geometric features as a result of the N-substituent modification. After a preliminary study of molecular modeling, cinnamoyl-, ...

A novel synthetic pathway towards the 2-oxazolidinone derivatives involving the halo-induced cyclisation of tert-butyl allyl(phenyl)carbamate was successfully developed. Various halogenating reagents were evaluated under different reaction conditions for the reaction optimisation. Interestingly,...

The ring contraction of trans-5-hydroxy-1,3-oxazin-2-ones 1 into cis-5-hydroxymethyl-oxazolidinones 3 was studied with different bases and nucleophiles and it was found that it is the basicity and not the nucleophilicity the factor responsible for the ring contractions. A DFT study was made for ...

The propensity for N-Boc-4-hydroxymethyl-oxazolidin-2-ones to undergo rapid O–O and N–O carbonyl transfer makes these l-serine derived chiral auxiliaries unsuitable for attachment to polymers.

All four stereoisomers of 5-formyl-4-hydroxymethyl-1,3-oxazolidin-2-ones (FHOs) were conveniently prepared from d-glucosamine by base-catalyzed epimerizations. 2-N,3-O-Carbonyl-d-glucosamine (7) was successively treated with NaBH4 and NaIO4 to give (4S,5R)-FHO 18, which was epimerized with DBU i...

Bromodomain protein 4 (BRD4) is a member of the bromodomain and extra-terminal domain (BET) protein family, which plays a key role in transcriptional regulation. Recent biological and pharmacological studies have enabled linking of the BET bromodomains with diseases, including inflammation and c...

A hypergraph H is said to be r-partite r-uniform if its vertex set V can be partitioned into non-empty sets V1,V2,...,Vr so that every edge in the edge set E(H), consists of precisely one vertex from each set Vi, i=1,2,…,r. It is denoted as Hr(V1,V2,…,Vr) or H(n1,n2,…,nr)r if |Vi|=ni for i=1,...

We compute the “norm” of irreducible uniformly bounded representations of SL(2,R). We show that the Kunze–Stein version of the uniformly bounded representations has minimal norm in its similarity class of uniformly bounded representations.

Case 2 (profile case) best–worst scaling (BWS) is a question-based survey method for measuring preferences for attribute levels. Several existing R packages help to implement the construction of Case 2 BWS questions (profiles) and the discrete choice analysis of the responses to the questions. ...

In this paper, a pybox-copper catalyzed enantioselective decarboxylative [4+2] cycloaddition reaction of ethynyl benzoxazinanones with azlactones has been developed, which provides optically active 3,4-dihydroquinolin-2-ones in high yields with good enantioselectivities and diastereoselectivitie...

A convenient synthesis of 2-(2-(difluoromethoxy)aryl)benzo[d]thiazoles from 2- (o-hydroxyaryl)benzothiazoles and commercially available ethyl difluoroiodoacetate (ICF2CO2Et) is described. The transformation was amenable to a one-pot, sequential three-component protocol from o-hydroxybenzaldehyde...

4-Bromo-3,4-dimethyl-1-phenyl-2-phospholene 1-oxide (3c) was first synthesized from 3,4-dimethyl-1-phenyl-2-phospholene 1-oxide (2c) by a bromo-radical substitution reaction occurred at C-4 position by N-bromosuccinimide and 2,2′-azobisisobutyronitrile. The novel phospha sugar analogue 3c exert...