Aryl morpholino-phosphoro:halide ester(s) - useful as phosphorylating agents

摘要

Phosphoric acid derivs. of formula (I) are new (where Ar is a substd. phenyl gp. derived from a phenol with a pKa of 7.5 or less; X is halogen). Phosphorylation of organic hydroxy cpds. (II) is effected by reacting (II) with (I). Cpds. (I) are esp. useful for phosphorylating nucleotides or polynucleotides in DNA or RNA synthesis. They have high selectivity for phosphorylating prim. OH gps. in the presence of sec. OH gps., and the Ar gp. is easily removed from the prod. under mild conditions. 4-Nitrophenyl morpholino phosphorochloridate (Ia) is specifically claimed.