On December 20, 2012, Atamanyuk, Dmytro; Denis, Alexis; Gerusz, Vincent; Ledoussal, Benoit; Bonvin, Yannick; Desroy, Nicolas; Gold, Johan; Moreau, Francois; Oxoby, Mayalen published a patent.Category: esters-buliding-blocks The title of the patent was Preparation of purine derivatives and their use as pharmaceuticals for prevention or treatment of bacterial infections. And the patent contained the following:
The invention relates to the compounds I [wherein A is Ph, naphthyl and 5-10 membered monocyclic or bicyclic unsaturated heterocycle, optionally substituted by a group R1 which is as defined in the application and is itself optionally substitutes by a group R2 which is as defined in the application and is itself optionally substituted by a group R3 which is defined in the application, Y and W, identical or different, are H, (C1-C6) alkyl, (C2-C6) alkenyl, (C2-C6) alkynyl, Ph or 4-10 monocyclic or bicyclic saturated or unsaturated heterocycle, optionally substituted by R1, or Y and/or W form a 4-10 membered cycle with R1, or Y and W form with N a saturated or unsaturated nitrogenous 4-10 membered mono, bi or tricyclic system, fused, bridged or spiro system, said system being optionally substituted by R1, said system being different from morpholine, with the proviso that when Y and A are Ph or heterocycle, W is not H] and their addition salts thereof with acids and bases. The invention also relates to a process and intermediates for their preparation and their use in the antibacterial prevention and therapy, used alone or in association with antibacterials, antivirulence agents or drugs reinforcing the host innate immunity, and pharmaceutical compositions and associations containing them. Thus, 6-[4-(methanesulfonyl)phenyl]purine II was prepared from 2,6-dichloro-9H-purine vis tetrahydropyranylation with 3,4-dihydro-2H-pyran in EtOAc containing catalytic PTSA; Suzuki coupling reaction with [4-(MeSO2)C6H4]B(OH)2 in aqueous DME containing K2CO3 and catalytic Pd(PPh3)4; amination with tert-Bu [(piperidin-4-yl)methyl]carbamate in MeCN containing DIPEA; and N-deprotection with HCl in THF/dioxane. The antibacterial activity of II was determined [IC50 = <300 μM vs. dltA gene of S. aureus]. The experimental process involved the reaction of tert-Butyl 7-benzyl-9-oxo-3,7-diazabicyclo[3.3.1]nonane-3-carboxylate(cas: 227940-70-7).Category: esters-buliding-blocks
The Article related to purine dimer derivative preparation antibacterial antivirulence agent immunomodulator, Biomolecules and Their Synthetic Analogs: Others, Including Purines, Pyrimidine Nucleic Acid Bases, Flavins, Lignans and other aspects.Category: esters-buliding-blocks
Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics