The Atherton‐Todd reaction was used for the preparation of a new class of hydrophilic drug carriers with an organic polyphosphate main chain. Chemical modification of poly(propy1ene phosphonate) (3) and poly(3,6,9‐trioxaundecamethylene phosphonate) (4) with benzocaine (ethyl 4‐aminobenzoate) (1) and phenethylamine (2) led in one step to polyphosphoramidates 7a, b and 8a, b bearing pharmacologically active amines in the side chain with modification yields of 60 to 75%.
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Brosse et al. (1989) studied this question.
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