摘要:
A process for recovering 3'-azido-3'-deoxythymidine (AZT) or a salt thereof from a mixture of chemicals involving the reaction of the AZT with guanidine to form a salt precipitate. The salt precipitate is then acidified to pH of less than about 9 to yield free AZT, which can then be crystallized from solution. 3'-Azido-3'-deoxythymidine and its salts, also known as AZT and Zidovudine, is used in the treatment of AIDS patients.
摘要:
A process from preparing 5-halogenated 2,3-O-cyclocytidine derivatives comprising reacting 2,3-O-cyclocytidine with a halogenating reagent, preferably N-bromosuccinimide, in the presence of an acid such as acetic or trifluoroacetic.
摘要:
A 5'-halo-2,3'-O-cyclocytidine of Formula I: ##STR1## wherein: X is a bromide, chloride, or iodide;Y is halide, sulfate, acetate, tosyl, mesyl, benzoate, and phosphate;R.sup.1 is hydrogen; andR.sup.2 is a hydroxy protecting group.Pharmaceutical compositions containing the above compounds exhibit antineoplastic activity.
摘要:
A composition of a 1:1 molar complex of guanidine and 3'-azido-3'-deoxythymidine (AZT) which is generated at about pH above 9 and disrupted by pH below about 9. This complex is a useful intermediate in the purification of AZT.
摘要:
Compounds of Formula IV: ##STR1## are described. In the compounds of Formula IV, R.sup.6 is selected from a trifluoromethyl group, a C.sub.1 -C.sub.6 alkyl group and a C.sub.6 -C.sub.9 aryl group, and R.sup.1 is selected from hydrogen, trityl, methoxytrityl, dimethoxytrityl, acetyl, a C2-C6 alkylacyl group, a C6-C9 arylacyl group, allyl, 2,2,2-trichloroethyl, phosphates and salts thereof, tosyl and mesyl. The above organosulfonyl salts of 2,3'-O-cyclocytidine are intermediates in the preparation of 1-(B-D-xylopentofuranose)cytosine, an inhibitor of DNA synthesis.
摘要:
A process for preparing 2,3'-O-cyclocytidine wherein 3'-deoxy-3'-organosulfonyl cytidine is refluxed in the absence of base. 2,3'-cyclocytidine is an intermediate in the preparation of 1-(B-D-xylo-pentofuranose) cytosine, an inhibitor of DNA synthesis.
摘要:
A compound of the formula A, wherein R* is a chiral auxiliary, and where the configuration at the asymmetric carbon atom between oxygen and sulfur is (R), (S), or combinations of (R) and (S), useful in the preparation of enantiomerically enriched 1,3-oxathiolane nucleoside analogues, for example (−)-FTC and 3TC.
摘要:
A process for the industrial scale manufacture of 4-(4-fluorophenyl)-N-alkylnipecotinate esters by the addition of 4-fluorophenylmagnesium halide in tetrahydrofuran to 3,4-unsaturated-3-piperidine esters.
摘要:
There are disclosed novel Stavudine solvates as follows: Stavudine NN-dimethyllacetamide solvates; Stavudine NN-dimethylacrylamide solvates and Stavudine NN-dimethylpropionamide solvates and processes for producing Stavudine NN-dimethylacetamide solvates, Stavudine NN dimethylacrylamide solvates and Stavudine NN dimethylpropionamide solvates which results in pure Stavudine.