Synthesis and biological activity of arylaliphatic N-(2-aminoethyl)-N-(2-hydroxy-2-phenylethyl)carboxamides

2-λ5-Phosphaquinolin-2-ones as Non-cytotoxic, Targetable, and pH-Stable Fluorophores

“…To determine whether the PN-scaffold was compatible with subcellular targeting approaches, we prepared heterocycle 8 (Scheme ) that integrates a lysosome-targeting morpholine unit and a consensus log(P o/w ) value of 4.75. , Ester hydrolysis of 3 gave the intermediate carboxylic acid 9 , which then underwent peptide coupling with HBTU and morpholine derivative 10 to afford 8 in modest yield. Slow diffusion of pentane into a concentrated solution of 8 in CHCl 3 gave single crystals suitable for X-ray diffraction.…”