专利号:US-2023174567-A1 优先权日:2020-05-22 标题:Synthesis of fluorinated nucleotides 发明人:ARMIGER TRAVIS; BELYK KEVIN M; BENKOVICS TAMAS; CHUNG CHEOL K; JI CHEN YINING; JOHNSON HEATHER CLAIRE; KLAPARS ARTIS; LIU ZHIJIAN; LIU ZHUQING; MOORE JEFFREY C; NEEL ANDREW J; PENG FENG; RUMMELT STEPHAN M; SALEHI MARZUARANI NASTARAN; SHERRY BENJAMIN D; SONG ZHIGUO JAKE; TURNBULL BEN WILLIAM HULME; WANG LU; XU FENG 权利人:MERCK SHARP & DOHME LLC 摘要:The present invention relates to efficient processes useful in the preparation of fluorinated nucleosides, such as (2S,3R,4S,5R)-5-(2-amino-6-oxo-1,6-dihydro-9H-purin-9-yl)-3-fluoro-4-hydroxy-2-(mercaptomethyl)tetrahydrofuran-3-yl dihydrogen phosphate, also known as 3′-fluoro-thio-guanosine monophosphate or 3′-F-thio-GMP. Such fluorinated nucleosides may be useful as a biologically active compound and or as an intermediate for the synthesis of more complex biologically active compounds. The present invention also encompasses intermediates useful in the disclosed synthetic processes and the methods of their preparation. (I)
专利号:US-7384739-B2 优先权日:2001-11-14 标题 :Compositions for enhancing DNA synthesis, DNA polymerase-related factors and utilization thereof 发明人:KITABAYASHI MASAO; KUROITA TOSHIHIRO; ISHIDA YOSHIKAZU; KOMATSUBARA HIDEYUKI; NISHIYA YOSHIAKI; OKA MASANORI; KAWAMURA YOSHIHISA; IMANAKA TADAYUKI 权利人:TOYO BOSEKI 摘要:The invention provides methods, kits, and compositions for enhancing synthesis of DNA involving a carboxylate ion-supplying substance that is effective in promoting DNA synthesis in enzymatic DNA synthesis reactions. The invention further provides a thermostable DNA polymerase-related factor derived from Thermococcus species, which has an activity to promote the DNA synthesis activity of DNA polymerase or which binds to DNA polymerase.
专利号:WO-2010144293-A1 优先权日:2009-06-08 标 题 :Synthesis of telcagepant and intermediates thereof 发明人:XU FENG; DESMOND RICHARD; HOERRNER R SCOTT; HUMPHREY GUY R; ITOH TETSUJI; JOURNET MICHEL; YOSHIKAWA NAOKI; ZACUTO MICHAEL J 权利人:MERCK SHARP & DOHME; XU FENG; DESMOND RICHARD; HOERRNER R SCOTT; HUMPHREY GUY R; ITOH TETSUJI; JOURNET MICHEL; YOSHIKAWA NAOKI; ZACUTO MICHAEL J 摘要:Disclosed is an efficient synthesis for the manufacture of the caprolactam intermediate (3R,6S)-3-amino-6-(2,3-difluorophenyl)-1-(2,2,2-trifluoroethyl)azepan-2-one: Formula and salts thereof, and an efficient preparation of telcagepant using the caprolactam intermediate.
专利号:WO-2019190945-A1 优先权日:2018-03-29 标 题 :Biosynthesis of olivetolic acid 发明人:GONZALEZ RAMON; TAN ZAIGAO; CLOMBURG JAMES M 权利人:UNIV RICE WILLIAM M 摘要:We present a biosynthetic approach to engineer novel microbes, such as Escherichia coli , for the production of olivetolic acid and other aromatic polyketides, as well as various downstream products that can be made therefrom. We engineered an E. coli strain that synthesizes olivetolic acid from a principle carbon source in vivo by expressing olivetolic acid synthase and olivetolic acid cyclase with the required modules of a β-oxidation reversal for hexanoyl-CoA generation. Further, we engineered an E. coli strain that synthesizes olivetolic acid which integrated additional auxiliary enzymes for increasing both hexanoyl-CoA and malonyl-CoA, enabling the synthesis of about 75 mg/L olivetolic acid and a productivity of 9.3 mg/hr olivetolic acid produced per gram dry weight of cells.
专利号:EP-0193420-B1 优先权日:1985-01-18 标题 :Device for the determination of compounds having an influence on the cellular oxidation pathway and methods for the determination of these compounds 摘要:1. Device for the specific assay of substrates, inhibitors, or activators of the cellular oxidation chain, characterized in that it contains an oxygen sensor, associated with means for measuring the oxygen detected, and the transporting species of the cellular respiratory chain in the form of immobilized bacteria, of immobilized microorganisms or of their immobilized membrane preparations, these cells having been cultured beforehand on a medium whose composition has produced a modification of the cellular synthesis of the flavoprotein corresponding to the compound to be assayed.
专利号:US-4283536-A 优先权日:1977-12-29 标 题:Preparation of vincadifformine and related derivatives 发明人:KUEHNE MARTIN E 权利人:UNIV VERMONT 摘要:This invention relates to the preparation of vincadifformine and related derivatives which are useful as starting material for the synthesis of among other alkaloids vincamine and other similar compounds possessing interesting psychopharmacologic properties. n A tetrahydro-β-carboline (II) is reacted with benzoyl chloride to provide a 2-benzoyl-1,2,3,4-tetrahydro-9H-pyrido-(3,4-b)-indole (III). Then compound (III) is reduced to give a 2-benzyl-1,2,3,4-tetrahydro-9H-pyrido-(3,4-b)-indole (IV). Thereafter, compound (IV) is transformed by t-butyl hypochlorite into a chloroindolenine derivative (V) which is immediately treated with a metal dialkylmalonate such as thallium t-butyl methyl malonate to give a dialkyl 3-benzyl-1,2,3,4,5,6-hexahydroazepino-(4,5-b)-indole-5,5-dicarboxylate (VI). Compound (VI) is then partly decarboxylated into a alkyl 3-benzyl-1,2,3,4,5,6-hexahydro-(4,5-b) indole-5-carboxylate (VII). Compound (VII) is hydrogenated to give an alkyl 1,2,3,4,5,6-hexahydroazepino-(4,5-b)-indole 5-carboxylate (VIII). In an alternative embodiment, compound (VI) can be hydrogenated to the corresponding dialkyl 1,2,3,4,5,6-hexahydroazepino-(4,5-b)-indole-5,5-dicarboxylate which is then decarboxylated into compound (VIII). Compound (VIII) is condensed with a functionalised aldehyde, typically a epoxy aldehyde or a haloaldehyde such as 1-bromo-4-formylhexane, to give vincadifformine or similar pentacyclic derivatives.
摘要:Journal of Pharmacy and Pharmacology., 17(814), 1965 [] 摘要:Journal of Biological Chemistry., 161(55), 1945 参考文献:10.1186/1752-153x-6-161 摘要:Zucca P, Rescigno A, Pintus M, Rinaldi AC, Sanjust E. Degradation of textile dyes using immobilized lignin peroxidase-like metalloporphines under mild experimental conditions. Chemistry Central Journal. 2012 Dec;6(1). doi: 10.1186/1752-153x-6-161. 参考文献:10.1007/s12010-012-0031-z 摘要:Jiang M, Ten Z, Ding S. Decolorization of Synthetic Dyes by Crude and Purified Laccases from Coprinus comatus Grown Under Different Cultures: The Role of Major Isoenzyme in Dyes Decolorization. Applied Biochemistry and Biotechnology. 2012 Dec 28;169(2):660–72. doi: 10.1007/s12010-012-0031-z.