Control of folding and binding of oligonucleotides by use of a nonnucleotide linker
摘要:
A linker containing a terephthalamide group, -P(O)(O-)O(CH2)6NHC(O)C6H4C(O)NH(CH2)6OP(O)(O-)-, is shown to be an effective structural element for organizing oligonucleotide chains in solution. Capping a pair of complementary oligonucleotides with this linker leads to marked enhancement in stability of the Watson-Crick duplex structure. Joining a pair of thymidylate oligomers with this linker gives a compound exhibiting unusually high affinity for oligo(dA) strands; even a tetramer unit can be recognized in dilute solution. Presumably Hoogsteen as well as Watson-Crick hydrogen bonding stabilizes a bimolecular 'triplex". Both types of linkage (i.e., joining two complementary strands and joining two pyrimidine strands) are embodied in the novel compound, d(TTTTTT-X-TTTTTT-X-AAAAAA), and function jointly in stabilizing a doubly folded monomolecular triple stranded structure (T(m) 58-degrees-C, 1 M NaCl; -X- represents the terephthalamide linker group).
Herein, we disclose a transition-metal-free reaction system that enables α-cyanation of sulfonamides through C–H bond cleavage for the preparation of α-amino nitriles, including difficult-to-access all-alkyl α-tertiary scaffolds. More than 50 substrate examples prove a wide functional group tolerance. Additionally, its synthetic practicality is highlighted by gram-scalability and the late-stage modification
A simple method for the synthesis of carbamate-protected guanidines from primary amines is described. A variety of thioureas derived from primary amines and isothiocyanates react with the Burgess reagent to give the corresponding guanidines via either a stepwise or one-pot procedure. By tuning the carbamoyl units of isothiocyanates and the Burgess reagent, differentially N,N′-diprotected guanidines
[EN] PYRIDINE DERIVATIVES AND METHODS OF USE<br/>[FR] DÉRIVÉS PYRIDINIQUES ET PROCÉDÉS D'UTILISATION
申请人:LINK TECHNOLOGIES LTD
公开号:WO2015132577A1
公开(公告)日:2015-09-11
The invention relates to compounds for use in the modification of compounds comprising nucleic acid sequences (such as oligonucleotides or the like), to modified oligonucleotides, to the delivery of modified oligonucleotides to cells and the like, and to the treatment of conditions by the delivery of modified oligonucleotides. The invention provides pyridine derived phosphoramidites, phosphorothioates, phosphate esters, solid supported equivalents, related oligonucleotides and the delivery of these to cells.
Design, Synthesis and Characterization of Pyrimidine based Thiazolidinedione Derivatives
作者:Vijay Kumar Sharma、Anup Barde、Sunita Rattan
DOI:10.14233/ajchem.2020.22565
日期:——
Novel thiazolidine-2,4-dione (TZD) based pyrimidine derivatives have been synthesized by Knoevenagel condensation reaction between thiazolidine-2,4-dione and amino pyrimidinyl aliphatic aldehydes followed by heterogeneous metal reduction. Synthetic strategy involved nucleophillic substitution of hydroxyl protected six membered aliphatic chain on 4,6-dichloropyrimidine followed by Suzuki coupling. This
(TFE) promoted synthesis of unsymmetric ureas was described. This approach enabled the construction of a variety of ureas from the readily prepared and easy-to-handle dioxazolones and amines viatandem Lossen rearrangement/condensation process. The reaction featured mild conditions for the urea synthesis under metal-free conditions, which was successively applied in the scale-up synthesis of herbicides