专利号:US-2003036066-A1 优先权日:2000-09-08 标 题:Linker phosphoramidites for oligonucleotide synthesis 发明人:PON RICHARD T; YU SHUYAN 权利人:UNIV TECHNOLOGIES INT 摘要:A novel approach for combining the ease of cleavage of carboxylic acid linker arms with the single phosphoramidite coupling chemistry of the universal supports useful in oligonucleotide synthesis. There is disclosed a new class of phosphoramidite reagents, linker phosphoramidites, which contain a bifunctional linker arm with a protected nucleoside linked through a 3′-ester bond on one end and a reactive phosphoramidite group or other phosphate precursor group on the other end—see FIGS. 2 and 3. The phosphoramidite group on the linker phosphoramidite may be activated under the same conditions and has similar reactivity as conventional nucleoside-3′-phosphoramidite reagents lacking the intermediate linker arm. The 3′-ester linkage contained within the linker phosphoramidite has similar properties to the linkages on prederivatized supports. The ester linkage is stable to all subsequent synthesis steps, but upon treatment with a cleavage reagent, such as ammonium hydroxide, the ester linkage is hydrolyzed. This releases the oligonucleotide product with the desired 3′-hydroxyl terminus and leaves the phosphate portion of the reagent attached to the support, which is subsequently discarded.
专利号:EP-0099068-B1 优先权日:1982-07-06 标题:Glycerine derivatives for phospholipids synthesis 摘要:New derivatives of glycerine having the formulas (I, II and III), wherein the symbol Z represents the methyl rest, a beta-unsaturated alkyl rest, an alkyl-aryl rest or a benzyl rest, or a cation equivalent, wherein the symbols R<1> and R<2>, being similar or different, represent a hydrogen atom, a rest R or an acyl rest -COR or a trityl rest with the proviso that it is in the position 1 or 3, wherein R represents an alkyl rest optionally unsaturated and/or substituted by halogen, hydroxy, carboxy, cyclo-alkyl or aryl, wherein the symbol X represents O, NH or N(R<3>) and the symbol R<3> when the symbol X represents O or NH represents an alkyl rest optionally unsaturated and/or substituted by halogen, amino, methyl-amino, dimethyl-amino, trimethyl-ammonio, hydroxy, carboxy, cyclo-alkyl or aryl, or when X is O, also D- or L-20-tert.-butyl-oxycarbonyl-amino-2-tert.-butyloxycarbonylethyl, 1,2- or 2,3-isopropylidene-dioxypropyl, 1,2-, 1,3 or 2,3-dibenzyloxy-propyl, 1,2,3,4,5-penta-benzyloxy-cyclohexyl or N-alkyl-amino-alkyl, or else when X is NH, also 1,2-dihydroxypropyl and when X is N(R<3>), of similar or different meaning, represent hydrogen or an alkyl rest optionally unsaturated and/or substituted by halogen, cyclo-alkyl or aryl. The compounds of the invention are valuable intermediates and have, at least partially, an anti-tumoral activity.
专利号:WO-8400367-A1 优先权日:1982-07-06 标 题 :New glycerine derivatives for the synthesis of phospholipides
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