A Search for Quantitative Acylation of α-Trinositol (1d-myo-Inositol 1,2,6-tris(dihydrogen phosphate) Pentasodium Salt)
摘要:
The acylation of alpha-trinositol is very sensitive to reaction conditions. Competing condensation reactions may give pyrophosphates and cyclic phosphates. Treatment of a tert-ammonium salt corresponding to alpha-trinositol with carboxylic acid anhydride and DMAP gives a good yield of the expected esters.
Heterobifunctional chemical linkers useful in protein degraders and other medicinal chemistry applications are provided. The heterobifunctional linkers include alkyne-piperidine and alkane-piperidine linkers; alkane- piperazine linkers; alkanamino PEGylated linkers; dipiperazine linkers; piperazine-pyridine/pyrimidine-alkyne linkers; pyridine-PEG-piperazine linkers and pyrimidine-piperazine-PEG linkers. Also provided are combinations of the provided linkers with a ligand that targets a degradation pathway, such as an E3 ubiquitin ligase enzyme.
The present invention relates to novel polyethylenamine-conjugated oligomeric compounds and to methods of making such compounds. The invention further relates to methods of enhancing the cellular uptake of oligomeric compounds comprising conjugating the compounds to fusogenic moieties such as polyethylenimine.