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Chapter 27,143

Phosphorylation of nucleoside derivatives with aryl phosphoramidochloridates

J.H. van Boom; P.M.J.B.rgers; R.C.ea; W.C.M.M.L.yten; A.B.J.V.nk; C.B.R.ese

Tetrahedron 31(23): 2953-2959

1975


ISSN/ISBN: 0040-4020
DOI: 10.1016/0040-4020(75)80318-8
Accession: 027142945

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The preparation of three aryl phosphorocyclohexylamidochloridates (7a, 7b and 7c) and an aryl phosphoromorpholidochloridate (8) is described. These aryl phosphoramidochloridates react with 2′,3′-O-methoxymethylene-uridine, -4-N-anisoylcytidine and -6-N-anisoyladenosine (9a, 9b and 9c, respectively), in the presence of the 1-ethylimidazole derivative (11a) to give high yields of the corresponding fully-protected 5′-phosphoramidates (10).

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