Process for the preparation of 5-substituted cytosines and other

Details Process for the preparation of 5-substituted cytosines and other Process for the preparation of 5-substituted cytosines and other

1992-11-19

1994-10-25

Ford, John M.

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

Organic compounds

Nitrogen attached directly or indirectly to the purine ring...

544309, 544314, C07D23936

Patent

active

053590678

ABSTRACT:
Process for the preparation of 5-substituted cytosines and other 4,5-disubstituted pyrimidin-2(1H)-ones, and intermediates arising in the course of this
The process for the preparation of compounds of the formula I, ##STR1## wherein compounds of the formula II ##STR2## are converted into an azole derivative of the formula III or an azine derivative of the formula IV ##STR3## which can subsequently be converted into a compound of the formula I using a nucleophile XH.

REFERENCES:
Some Pyrimidine Derivatives, J. L. Rabinowitz et al., J. Am. Chem. Soc., 75:5758-5759 (1953).
Synthesis of N-(2,3-Dihydroxypropyl) Derivatives of Nucleic Bases, Ueda et al., J. Heterocyclic Chem., 8:827-829 (1971).
Chemical Conversion of Thymidine Into 5-Methyl-2'-deoxycytidine, W. L. Sung, J.C.S. Chem., Comm. 1089 (1981).
4-(1,2,4-Triazol-1-yl)- and 4-(3-Nitro-1,2,4-triazol-1-yl)-1-(.beta.-D-2,3,5-tri-O-acetylarabinofurano syl)pyrimidin-2(1H)-ones. Valuable Intermediates in The Synthesis of Derivatives of 1-(.beta.-D-Arabinofuranosyl)cytosine (Ara-C), K. J. Divakar et al., J.C.S. Perkin I, 1171-1176 (1982).
Studies of Antitumor-Active 5-Fluorouracil Derivatives. I. Synthesis of N-Phthalidyl 5-Fluorouracil Derivatives, S. Kamata et al., Chem. Pharm. Bull., 33(8):3160-3175 (1985).
Grabowicz et al., 5-Fluorocytosine from 5-fluorouracil, Chemical Abstracts, vol. 100, 1984, p. 602, abstract No. 209860h.
Jahne et al., Preparation of Carbocyclic Phosphonate Nucleosides, Tetrahedron Letters, vol. 33, No. 37, pp. 5335-5338, 1992.

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