CAS: 59456-70-1; (S)-2-((2S,3S,4S)-2-Amino-4-Hydroxy-4-(5-Hydroxypyridin-2-yl)-3-Methylbutanamido)-2-((2R,3S,4R,5R)-5-(2,4-Dioxo-3,4-Dihydropyrimidin-1(2H)-yl)-3,4-Dihydroxytetrahydrofuran-2-yl)Acetic Acid

上下游产品

(+/-)-2-Benzyloxycarbonylamino-4-[2-(5-Benzyloxypyridyl)]-4-Tert-Butyldimethylsilyloxy-3-Methylbutanoic Acid

📜在 钯 N-甲基吗啉,甲醇,甲酸,Oxalylditriazole,水,Potassium Carbonate体系中,用 四氢呋喃 作为反应溶剂,化学反应 53.5H,反应生成 华光霉素
参考文献:A Synthesis Of Nikkomycin Z: Improved Synthesis And Protection Of The Pyridyl γ-Hydroxy-α-Aminobutanoic Acid Component
标题:A Synthesis Of Nikkomycin Z: Improved Synthesis And Protection Of The Pyridyl γ-Hydroxy-α-Aminobutanoic Acid Component
摘要:The First Synthesis Of Nikkomycin Z Is Described. An Improvement Of The Isoxazoline-Based Methodology6,12 And An Effective Method For Protection Of Lb Were Devised. The Application Of Oxalyditriazole (23) For Peptide Coupling Proved Most Effective In Completing The Synthesis. A New And Efficient Synthesis Of The Prerequisite Pyridyl E-Olefin (5) Is Also Described.
DOI:10.1016/s0040-4039(00)73678-1

专利信息

专利号:US-2005080260-A1
优先权日:2003-04-22
标 题 :Preparation of prodrugs for selective drug delivery
发明人：MILLS RANDELL L; WU GUO-ZHANG
摘要:Synthesis of a chemical compound having the formula A-B-C that may serve for applications such as drug delivery where A is a chemiluminescent, moiety, B is a photochromic moiety, and C is a biologically active moiety where A-B-C may serve as a prodrug. Novel synthetic methods of the present invention to form the prodrug comprised the steps of (1) forming a benzophenone, (2) forming a diaryl ethylene, (3) attaching a phthalimide moiety to at least one of the aryl groups of the ethylene to form a phthalimide-ethylene conjugate, (4) condensing two ethylene-phthalimide conjugates to form a phthalimide-pentadiene conjugate, (5) converting the phthalimide to the phthalhydrazide by reaction with hydrazine to form a carrier compound according to the present invention, and (6) reacting the carrier compound with an nucleophilic moiety of the drug to form the corresponding prodrug. Alternatively the carrier can be prepared by using the halo-substituted diaryl ethylene to make the corresponding cationic leuco dye-like compound with known methods. The cationic compound then is protected by reacting with a nucleophile and coupled with the aminophathalimide by palladium-catalyzed amination to form the protected phthalimide-pentadiene conjugate. The latter is refluxed with hydrazine to convert its phthalimide to the phthalhydrazide and acidified to give the carrier. An additional aspect of the present invention relates to the use of these compounds as antiviral agents for the treatment of viral infections such as HIV and as anticancer agents for the treatment of cancers such as bowel, lung, and breast cancer.

专利号:WO-9967419-A1
优先权日:1998-06-25
标题 :β(1,6)-GLUCAN SYNTHESIS AND CELL WALL ASSEMBLY ASSAY
发明人：OSTROFF GARY R
权利人:COLLABORATIVE GROUP LTD; OSTROFF GARY R
摘要:Methods are disclosed for assessing an agent for an ability to inhibit β(1,6)-glucan synthesis and/or incorporation of β(1,6)-glucan into the cell wall, comprising contacting samples of yeast cells that are sensitive to a killer toxin that targets β(1,6)-glucan with a test agent and a lethal dose of the killer toxin, and/or contacting samples of yeast cells that are sensitive to the killer toxin with a test agent and a sublethal dose of the killer toxin, and assessing the permeability of the cells in the samples, such as by using a membrane-impermeable dye that fluoresces on contact with DNA.

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:US-5433947-A
优先权日:1992-12-15
标 题 :Antifungal synergistic combination of enzyme fungicide and non-enzymatic fungicide and use thereof
发明人：HARMAN GARY E; LORITO MATTEO; PIETRO ANTONIO D; HAYES CHRISTOPHER K
权利人:CORNELL RES FOUNDATION INC
摘要:Antifungal composition comprising synergistic combination of fungal cell wall degrading enzyme selected from the , group consisting of chitinolytic enzymes, glucanolytic enzymes and cellulases and non-enzymatic fungicides selected from the group consisting of sterol synthesis inhibiting fungicides (e.g., flusilazole and miconazole) and thiol group inactivating fungicides which are not specific to fungal cell membranes (e.g., captan) are applied in an antifungal effective amount to fungus to be inhibited or to a locus to be protected from said fungus.

专利号:JP-2007520565-A
优先权日:2004-02-04
标题 :Synthesis of dehydrophenylahistine and their analogs, and dehydrophenylahistine and their analogs

专利号:CN-101633655-B
优先权日:2002-08-02
标题 :Dehydrophenylahistine and its analogues and synthesis of dehydrophenylahistine and its analogues