CAS: 24751-69-7; ((2S,3S,4R,5R)-5-(6-Amino-9H-Purin-9-yl)-2-Fluoro-3,4-Dihydroxytetrahydrofuran-2-yl)Methyl Sulfamate

专利信息

专利号:US-2007065922-A1
优先权日:2005-09-21
标题 :Biocatalytic synthesis of aminodeoxy purine N9-beta-D-nucleosides containing 3-amino-3-deoxy-beta-D-ribofuranose, 3-amino-2,3-dideoxy-beta-D-ribofuranose, and 2-amino-2-deoxy-beta-D-ribofuranose as sugar moieties
发明人：BARAI VLADIMIR N; EROSHEVSKAYA LUDMILLA A; MIKHAILOPULO IGOR A; AZHAYEV ALEX V; LAPINJOKI SEPPO P
权利人:METKINEN OY
摘要:Purine N 9 -β-D-nucleosides containing 3-amino-3-deoxy-β-D-ribofaranose, 3-amino-2,3-dideoxy-β-D-ribofuranose, and 2-amino-2-deoxy-β-D-ribofuranose as sugar moieties are synthesized by biocatalytic transglycosylation of purine bases and the respective 3′-amino-3′-deoxyuridine, 3′-amino-3′-deoxythymidine and 2′-amino-2′-deoxyuridine as donors of the carbohydrate moiety, and the cells of Escherichia coli as a biocatalyst or glutaraldehyde (GA) treated cells of Escherichia coli as a biocatalyst or a mixture of thymidine (uridine) phosphorylase and purine nucleoside phosphorylase.

专利号:WO-2021140471-A1
优先权日:2020-01-10
标题:Method for synthesis of 2'-alkyl- or 2'-alkenyl- or 2'-alkynyl-4'-fluoro-adenosine derivatives and intermediates thereof
发明人：ZHANG HAI-REN; SEREBRYANY VLADIMIR
权利人:JANSSEN BIOPHARMA INC
摘要:A method of making nucleoside 1, which has a 3-hydrocarbyl-5-fluoro-5-(hydroxy-methyl)tetrahydrofuran-3,4-diol ring system, where hydrocarbyl group R1 is lower alkyl, lower alkenyl, or lower alkynyl and R2 may be an adenine moiety having an exocyclic amino group protected as an imidodicarbonate or as a carbamate. Nucleoside 1 is prepared from an intermediate 4 by adding iodine fluoride across the exocyclic double bond to produce a 5-fluoro-5-iodomethyl derivative 5. The iodine atom is displaced with a carboxylic acid nucleophile in the presence of an oxidizing agent to produce a 5-fluoro-5-(acyloxy)methyl ester derivative 7, where R 3 is an acyl group. Ester 7 may be converted into compound 1 by cleavage of the ester.

专利号:EP-0635577-B1
优先权日:1993-07-23
标 题 :Screen for inhibitors of melanin biosynthesis
发明人：BRINDLE FRANCES HARRIET ELIZAB; FROELIGER EUNICE HARRIET
权利人:BASF AG
摘要:A method for the identification of agents that inhibit melanin biosynthesis involves the incubation of test samples in cultures of a fungus that produces melanin. Observation of altered pigmentation in the culture or culture area containing test sample indicates inhibition of melanin biosynthesis. Preferred cultures for the screen contain a fungus that pigments in the light or the dark such as Cladosporium cucumerinum. Preferred embodiments employ test samples on disks or in wells in solidified cultures and a known melanin synthesis inhibitor as a positive control which is compared to the test sample by simple visual inspection.

专利号:WO-2009058800-A2
优先权日:2007-10-29
标题:Synthesis of nucleosides

专利号:US-6589762-B1
优先权日:1993-05-25
标 题:Calcafluor screen for chitin biosynthesis inhibitors
发明人：KIRSCH DONALD RICHARD; KUH LAI MARGARET HSIEN-FEN; SILVERMAN SANFORD J
权利人:BASF AG
摘要:A method for the identification of agents which inhibit chitin synthesis, thus exhibiting potential fungicidal and insecticidal activity, involves the incubation of test samples in neutral Saccharomyces cerevisiae cultures containing calcofluor white, a fluorochrome that causes lethal chitin hyper-polymerization in the yeast. Cultures containing samples that inhibit chitin synthesis exhibit enhanced growth because the growing fungus is rescued from the adverse effects of calcofluor white. In the practice of the invention, the test sample is added to a S. cerevisiae culture or culture area containing calcofluor white and the culture is incubated with the test sample for such time under such conditions sufficient to observe yeast cell growth inhibition in a corresponding culture or culture area containing calcofluor but no test sample. The extent of growth in the culture or culture area containing test sample is then compared with the extent of growth in the culture or culture area containing no test sample, and the presence of chitin synthesis inhibition is determined by observation of whether culture growth in the presence of test sample exceeds growth in its absence. Preferred embodiments employ test samples on disks or in wells in solidified cultures and a known chitin synthesis inhibitor as a positive control which is compared to the test sample.

专利号:JP-S584780-A
优先权日:1981-06-29
标题:Synthesis method of 4',5'-unsaturated nucleosides