专利号:US-7160517-B2 优先权日:2000-08-18 标题 :Apparatus and methods for the automated synthesis of oligosaccharides 发明人:SEEBERGER PETER H; PLANTE OBADIAH J 权利人:MASSACHUSETTS INST OF TECHNOLG 摘要:One aspect of the present invention relates to an apparatus for the efficient synthesis of oligosaccharides on a solid support, e.g., formed by subunit addition to terminal subunits immobilized on solid-phase particles. In certain embodiments, the apparatus of the present invention is used in combinatorial methods, e.g., as described herein, of synthesizing oligosaccharides.
专利号:US-6048975-A 优先权日:1991-09-12 标 题:Process for the chemical synthesis of oligonucleotides 发明人:PFLEIDERER WOLFGANG; BERGMANN FRANK 权利人:HOECHST AG 摘要:A process for the chemical synthesis of oligonucleotides n Use of a dansylethoxycarbonyl group as base-labile 5'-hydroxyl protective group in the chemical synthesis of DNA and RNA and suitable synthetic processes. n The ease of detection of the dansyl protective group and the ease of elimination from the sugar residue of the nucleotide without side reactions make oligonucleotide synthesis possible with high yields in very small quantities.
专利号:WO-2014148928-A1 优先权日:2013-03-21 标 题:Method for incorporating protecting acetal and acetal ester groups, and its application for the protection of hydroxyl function 发明人:MARKIEWICZ WOJCIECH; TOÅš-MARCINIAK AGNIESZKA; CHMIELEWSKI MARCIN 权利人:INST CHEMII BIOORG POLSKIEJ AKADEMII NAUK 摘要:The present invention is the method for incorporation of acetal and acetal ester groups for protection of hydroxyl function. The method is applied in particular in the processes of RNA synthesis. The method can be employed in the synthesis of nucleosides with acetal and acetal ester groups for the protection of hydroxyl functions. The method according to the invention consists of the reaction of an organic compound containing at least one hydroxyl group, soluble in an aprotic solvent, with a compound of the general formula 1, R 1 -S-CH 2 -O-R 2 (1) in the presence of SnCl 4 , in an aprotic solvent. In the second aspect, the present invention is the method of protecting the hydroxyl function, particularly in position 2', in nucleoside derivatives, based on the incorporation of an acetal or acetal ester group.
专利号:US-3950389-A 优先权日:1968-10-04 标 题 :Stereospecific total steroidal synthesis via substituted C/D-trans indanones 发明人:HAJOS ZOLTAN GEORGE 权利人:HOFFMANN LA ROCHE 摘要:Total synthesis of known progestationally active steroidal materials. The steroids can be synthesized depending on the particular starting reactants selected by employing as intermediates bicyclic compounds of the formula ##SPC1## n Wherein m is an integer having a value of 1 or 2; R 4 is hydrogen or lower alkyl; Z is lower alkylenedioxymethylene CH(OR 2 ) and carbonyl; R 8 when taken alone is hydrogen; R 9 when taken alone is lower alkoxycarbonyl, aryloxy-carbonyl, lower cycloalkyloxycarbonyl, carbonyl-halide, hydrogen, carboxy, formyl and methylene-X, where X is a leaving group and when taken together are methylene; with the proviso that when Z is carbonyl R 8 when taken alone is hydrogen; R 9 when taken alone is carbonyl halide, hydrogen, carboxy, formyl and methylene-X where X is a leaving group and when taken together are methylene and R 2 is hydrogen, lower alkyl, lower alkoxy-lower alkyl, phenyl-lower alkyl, tetrahydropyranyl, lower alkanoyl, benzoyl, nitrobenzoyl, carboxy-lower alkanoyl, carboxybenzoyl, trifluoroacetyl and camphorsulfonyl n And reacting them in the case where R 8 and R 9 taken together are methylene or R 8 is hydrogen and R 9 is methylene-X with β-keto esters and other analogs of the formula ##EQU1## wherein R.sub. 6 is selected from the group CONSISTING OF ##EQU2## and LOWER ALKYL; R 7 is lower alkyl; R 15 is selected from the group consisting of oxo, lower alkylene-dioxy or (hydrogen and lower alkoxy); B is selected from the group consisting of lower alkoxy-carbonyl-methylene, lower-aryloxy-carbonyl-methylene, cyanomethylene, lower alkyl sulfinyl-methylene, lower alkyl sulfonyl-methylene, and R 25 and R 26 are independently selected from the group consisting of hydrogen, hydroxyl and lower alkyl.
专利号:US-7019131-B2 优先权日:1998-08-10 标 题:Programmable one-pot oligosaccharide synthesis 发明人:WONG CHI-HUEY; ZHANG ZHIYUAN; OLLMANN IAN; BAASOV TIMOR; YE XIN-SHAN 权利人:SCRIPPS RESEARCH INST 摘要:The reactivity of a number of p-methylphenyl thioglycoside (STol) donors which are either fully protected or have one hydroxyl group exposed has been quantitatively determined by HPLC in conjunction with the development of a broadly applicable approach for a facile one-pot synthesis of oligosaccharides. The influence on reactivity of the structural effects of different monosaccharide cores and different protecting groups on each glycoside donor is characterized and quantified. In addition, a correlation between glycosyl donor reactivity and the chemical shift of the anomeric proton by 1 H NMR has been established. A database of thioglycosides as glycosyl donors has been created using this reactivity data. The utility is demonstrated by the easy and rapid one-pot assembly of various linear and branched oligosaccharide structures. In addition, a computer program as been described for use as a database search tool and guide for the selection of building blocks for the one-pot assembly of a desired oligosaccharide or a library of individual oligosaccharides.
专利号:US-2004110228-A1 优先权日:2002-04-01 标 题:Combinatorial organic synthesis of unique biologically active compounds 发明人:MCALPINE SHELLI R; TAYLOR RACHEL E; BOLLA MEGAN L; SEGALL ANCA M 摘要:The invention provides a method for making a combinatorial library of cyclic compounds, such as Holliday junction-trapping compounds, comprising the steps of (a) obtaining a plurality of trimers according to the generic structure X 1- X 2- X 3 , wherein X 1 , X 2 and X 3 can be independently any naturally or nonnaturally occurring amino acids or peptidomimetics thereof; (b) optionally coupling a spacer S to the trimer at either end; (c) cyclizing two trimers or trimer-spacer conjugates in a head-to-tail orientation; thereby obtaining a combinatorial library of compounds, wherein the library does not include an unmodifed or naturally occurring Holliday Junction-trapping compounds. The invention additionally provides methods macrocyclic compounds that are synergimycin derivatives.