专利号:US-11603382-B2 优先权日:2015-12-11 标题 :Diastereoselective synthesis of phosphate derivatives 发明人:KOTALA MANI BUSHAN; DAMMALAPATI VENKATA LAKSHMI NARASIMHA RAO 权利人:NuCana plc 摘要:The present invention provides a method for the preparation of intermediates useful in the synthesis of gemcitabine-[phenyl-benzoxy-L-alaninyl)]-phosphate. It also provides a method of preparing gemcitabine-[phenyl-benzoxy-L-alaninyl)]-phosphate.
专利号:US-4780504-A 优先权日:1985-06-20 标 题 :Supports useful in solid phase synthesis of oligonucleotides 发明人:BUENDIA JEAN; NIERAT JEANINE 权利人:ROUSSEL UCLAF 摘要:Novel supports useful in solid phase synthesis of oligonucleotides of the formula I +TR wherein &cir& is micro pellets of a material selected from the group consisting of glass, silica, Kieselguhr, polytetrafluoroethylene, cellulose and metallic oxides, m is an integer from 1 to 20, A is selected from the group consisting of alkylene of 1 to 20 carbon atoms, saturated cycloalkylene of 3 to 12 carbon atoms, phenyl and 5 to 6 member heterocycles, x is an integer from 0 to 20, x1 is an integer from 0 to 10 and the amino group may be in the m-, p- or o-position, a process for the preparation of said supports, the use of said supports and intermediates.
专利号:US-10995093-B2 优先权日:2016-04-07 标 题 :Synthesis of 2′-fluoro-6′-methylene-carbocyclic adenosine (FMCA) and 2′-fluoro-6′methylene-carbocyclic guanosine (FMCG) 发明人:CHU CHUNG K; MULAMOOTTTIL VARUGHESE ALEXANDER; MISHRA RAM C; SINGH UMA SHARAN 权利人:UNIV GEORGIA 摘要:The invention provides a new convergent approach for the synthesis of 2′-fluoro-6′-methylene-carbocyclic adenosine (FMCA) and 2′-fluoro-6′-methylene-carbocyclic guanosine (FMCG) from a readily available starting material in eight steps. An efficient and practical methodology for stereospecific preparation of a versatile carbocyclic key intermediate, (1S,3R, 4R)-3-tert-butoxy-4-(tert-butoxymethyl)-2-fluoro-5-methylenecyclopentanol (compound 8 of scheme 1A or a) in only six (6) steps is also provided. Prodrugs of these compounds are also prepared.
专利号:US-11744150-B2 优先权日:2012-01-20 标 题:Synthesis of aza-acenes as novel n-type materials for organic electronics 发明人:THOMPSON MARK E; SOMMER JONATHAN R; BARTYNSKI ANDREW 权利人:UNIV SOUTHERN CALIFORNIA 摘要:Acenes, such as aza-acenes are attractive materials for organic semiconductors, specifically for n-type materials. There are disclosed new derivatives of acenes that are fabricated using novel synthesis. For example, the disclosed fabrication strategies have allowed for the first time new aza-tetracene and aza-pentacene derivatives. The HOMO and LUMO energy levels of these materials are tunable through appropriate substitution and as predicted, deepened. There are also disclosed organic photosensitive devices comprising at least one aza-acene such as aza-tetracene and aza-pentacene.
专利号:US-7078572-B2 优先权日:2002-09-20 标题:Process for the synthesis of intermediates useful for the synthesis of tubulin inhibitors 发明人:KENDALL JOHN THOMAS 权利人:WYETH CORP 摘要:The invention is a process for the preparation of compounds of the Formula I: n nwhere R 1 , R 2 , R 3 , R 4 and R 5 are defined in the specification, which are intermediates useful for the preparation of tubulin inhibitors which are useful in the treatment of cancer.
专利号:US-7091334-B2 优先权日:1997-07-25 标题 :Method for large-scale production of di(uridine 5′)-tetraphosphate and salts thereof 发明人:YERXA BENJAMIN R; PENDERGAST WILLIAM 权利人:INSPIRE PHARMACEUTICALS INC 摘要:The present invention provides new methods for the synthesis of the therapeutic dinucleotide, P 1 ,P 4 -di(uridine 5′)-tetraphosphate, and demonstrates applicability to the production of large quantities. The methods of the present invention substantially reduce the time period required to synthesize diuridine tetraphosphate, preferably to three days or less. The novel tetrammonium and tetrasodium salts of P 1 ,P 4 -di(uridine 5′)-tetraphosphate (Formula I) prepared by these methods are stable, soluble, nontoxic, and easy to handle during manufacture. n nwherein:n X is Na, NH 4 or H, provided that all X groups are not H.
[参考文献]: R M Dawson, Et Al. Phenyldichlorophosphate As An Aid In Studies Of Decarbamylation Of Carbamylated Acetylcholinesterase. Anal Biochem. 1988 May 1;170(2):451-5.
合成参考文献
摘要:Mérour, J.-Y.; Joseph, B., Science of Synthesis Knowledge Updates, (2016) 3, 176. 摘要:Gigiena i Sanitariya. For English translation, see HYSAAV., 39(4)(86), 1974