A broad-spectrum, catalytic method has been developed for the synthesis of sulfonamides and sulfamates. With activation by combination a amount 1-hydroxybenzotriazole (HOBt) silicon additives, amidations sulfonyl fluorides fluorosulfates proceeded smoothly excellent yields were generally obtained (87%-99%). Noticeably, this protocol is particularly efficient sterically hindered substrates. Cata...

L-aspartic acid building blocks bearing galactosyl moieties were used to synthesise glycolipid mimetics of variable hydrocarbon chain length. The glycolipids were readily prepared through amide bond formation using the TBTU/HOBt coupling methodology. It was observed that, under these conditions, activation of the α-carboxylic acid of the intermediates led to near complete racemisation of the ch...

Peptide derivatives of Aspirin (1 to 8) were synthesized by using Ac2O/AcOH reaction with Salicyclic acid. Aspirin was coupled with amino acid amide and dipeptide amide and tripeptide amide using its p-nitro phenyl (NP) ester. The ester (Aspirin–ONP) was prepared using p-nitro phenol and DCC in EtOAc and was precipitated using EtOH. The synthesis of dipeptide amides were carried out in solution...

Ethenetricarboxylic acid diester 1a is a useful compound bearing two reactive sites, a CO2H group and a Michael acceptor. Reactions of 1a and reagents with oxygen and nitrogen nucleophilic moieties have been examined. The reaction of 1a with 2-aminoalcohols in the presence of EDCI and HOBt in one pot gave N,O-containing heterocyclic compounds, regioselectively. The stepwise method has also been...

All Fmoc (9-fluorenylmethoxycarbonyl) protected amino acids, NovaSyn TG Sieber resin, and coupling reagents (HOBt, 1-Hydroxybenzotriazole, HATU, 1-[Bis(dimethylamino)methylene]-1H-1,2,3-triazolo[4,5b]pyridinium 3-oxid hexafluorophosphate, and PyBOP, (Benzotriazol-1-yloxy)tripyrrolidinophosphonium hexafluorophosphate) were purchased from Novabiochem. All solvents, used in the synthesis and purif...

Hyperbaric oxygen therapy (HBOT) has been shown to be efficacious in treating various conditions, including perianal Crohn's disease. Here we present a case of a 59-year-old male with a history of ulcerative colitis, who underwent a total proctocolectomy and two-stage J-pouch construction. He later developed chronic antibiotic-refractory pouchitis with endoscopic features of ischemia. At the co...