The present invention relates to nitric oxide donor carnosine derivatives having a great efficacy in reducing elevated intraocular pressure, to processes for their preparation and to their use in the treatment and/or prophylaxis of glaucoma and ocular hypertension.
The present invention relates to nitric oxide donor carnosine derivatives having a great efficacy in reducing elevated intraocular pressure, to processes for their preparation and to their use in the treatment and/or prophylaxis of glaucoma and ocular hypertension.
The present invention relates to 15-nitrooxyderivatives of fluprostenol, their use for the treatment of glaucoma and ocular hypertension and formulation containing 15-nitrooxy derivatives of fluprostenol.
The solid-phase preparation of oligodeoxyribonucleotides attached to intercalator or reactive groups through their 5'- and (or) 3'-ends is reported. These syntheses implicate the introduction of suitable masked functional groups at the 5'-end of the oligonucleotide by the intermediate of their phosphoramidite derivatives or at the 3'-end of the oligonucleotide using modified solid supports. After full deblocking, the functional groups (phosphate, thiophosphate, primary amine or thiol) can be reacted with the suitable reactive group involved in the chosen ligand. These methods allow the preparation of heterobifunctional derivatized oligodeoxyribonucleotides.
Organocatalytic Activation of Alkylacetic Esters as Enolate Precursors to React with α,β-Unsaturated Imines
作者:Lin Hao、Shaojin Chen、Jianfeng Xu、Bhoopendra Tiwari、Zhenqian Fu、Tong Li、Jieyan Lim、Yonggui Robin Chi
DOI:10.1021/ol4021805
日期:2013.10.4
Asymmetric functionalization of alkylacetic esters and their derivatives is traditionally achieved via preformed enolates with chiral auxiliaries. Catalytic versions of such transformations are attractive but challenging. A direct catalytic activation of simple alkylacetic esters via N-heterocyclic carbene organocatalysts to generate chiral enolate intermediates for highly enantioselective reactions is reported.