Novel nucleoside-phospholipid conjugate

Details Novel nucleoside-phospholipid conjugate Novel nucleoside-phospholipid conjugate

1989-11-28

1991-09-24

Brown, Johnnie R.

Organic compounds -- part of the class 532-570 series

Organic compounds

Carbohydrates or derivatives

536 27, 536 28, C07H 1910, C07H 1920, C07D47300

Patent

active

050514997

ABSTRACT:
Novel nucleoside-phospholipid conjugates of the formula ##STR1## wherein R.sub.1 is C.sub.14-24 long chain aliphatic acyl or C.sub.1-24 aliphatic alkyl, R.sub.2 is C.sub.2-10 aliphatic acyl or C.sub.1-24 aliphatic alkyl and N.sub.s is a nucleoside residue; and pharmacologically acceptable salts thereof are prepared in a one-step reaction by reacting the corresponding nucleoside and glycerophospholipid derivative in the presence of phospholipase D-P.

REFERENCES:
patent: 4291024 (1981-09-01), Turcotte
patent: 4797479 (1989-01-01), Shuto
patent: 4921951 (1990-05-01), Shuto
"Phospholipid Derivatives of Necleoside Analogs as Prodrugs with Enhanced Catabolic Stability", Cancer Research, vol. 41, Jul. 1981, by T. Matsushita et al., pp. 2707-2713.
"Cytotoxic Liponucleotide Analogs", Biochimica et Biophysica Acta, 619, 1980, by J. G. Turcotte et al., pp. 619-631.
"Synthesis of Phospholiponucleosides", Synthesis, May 1982, by Fausto Ramirez et al., pp. 402-404.

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