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classificationCPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07H19-12
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filingDate 1972-05-01-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationDate 1975-05-29-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber GB-1395764-A
titleOfInvention Cytidines and related compounds
abstract 1395764 A process for preparing cytidines and some related compounds and some novel products thereof SCHERING AG 1 May 1972 [4 May 1971] 20115/72 Heading C2C A process for preparing compounds of the Formula I wherein R 1 and R 2 each is hydrogen or alkyl or R 1 is hydrogen and R 2 is hydroxy or amino or alkyl which is terminally substituted, or R 1 and R 2 together with the adjacent nitrogen is a 4-, 5-, 6- or 7-membered heterocyclic ring which may contain a further hetero atom; R 3 is hydrogen, halogen or C 1-6 alkyl; X is oxygen or sulphur; Y is nitrogen or CH and Z is a free or protected sugar group comprises reacting a compound II wherein "alkyl" is a C 1-6 alkyl group and Z<SP>1</SP> is a silylated or acylated sugar group with ammonia or an amine R 1 R 2 NH or, in the presence of a tertiary base, a salt of an amine R 1 R 2 NH and optionally removing the protective group(s) on the sugar group and further optionally converting the free sugar group to a protected sugar group. The compound II may be generated in situ by reacting a compound III with hexamethyldisilazane in the presence of trimethyl chlorosilane or an ammonium salt. The novel compounds are of the Formula I in which R 1 is H and R 2 is amino, aralkyl having at least two carbon atoms in the alkyl moiety and which is unsubstituted or substituted in aryl moiety or an N-substituted aminoalkyl or R 1 and R 2 together with the nitrogen atoms form a 4-, 5-, 6- or 7-membered ring which may contain a further hetero atom, R 3 , X and Y are as defined above, and Z is a free or protected sugar group other than an arabinofuranosyl group. The intermediate, of the Formula II may be prepared by condensing a compound II in which Z<SP>1</SP> is hydrogen with a suitable sugar. Pharmaceutical compositions of the compounds I show anti-metabolite and anti-tumour activity.
priorityDate 1971-05-04-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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Total number of triples: 35.