4-甲氧基苯基溴化镁置于乙醚,苯体系中,化学反应生成4-甲氧基三苯基氯甲烷 参考文献:The Dissociation Of Hexaarylethanes.1 Xv. Methoxyl Substituents 标题:The Dissociation Of Hexaarylethanes.1 Xv. Methoxyl Substituents 摘要: Doi:10.1021/ja01231A032
专利号:US-2008287649-A1 优先权日:2006-12-29 标 题 :Methods for the synthesis of cyclic peptides 发明人:CHEN LIN; HAN YEUN-KWEI; ROBERTS CHRISTOPHER R 权利人:CHEN LIN; HAN YEUN-KWEI; ROBERTS CHRISTOPHER R 摘要:Methods for the synthesis of cyclic peptides are provided, as well as novel dipeptide compounds. The methods include the solid phase synthesis of a dipeptide, which is the coupled to a second peptide in a solid phase reaction. The peptide is then cyclized following the coupling reaction. The methods and dipeptides are particularly useful for the synthesis of MC-4 receptor agonist peptides.
专利号:US-8138330-B2 优先权日:2006-09-11 标 题 :Process for the synthesis of oligonucleotides 发明人:LEUCK MICHAEL; WOLTER ANDREAS; STUMPE ALFRED 权利人:LEUCK MICHAEL; WOLTER ANDREAS; STUMPE ALFRED; SIGMA ALDRICH CO LLC 摘要:The present invention discloses novel methods for the synthesis of oligonucleotides with nucleoside phosphoramidites on solid supports. The methods comprise the stepwise chain assembly of oligonucleotides on supports with 5′-acyl phosphoramidites. The synthesis cycles consist of a front end deprotection step which is conducted with a solution of a primary amine or a phenolate, a phosphoramidite coupling step with a 5′-acyl nucleoside phosphoramidite in the presence of an activator, a phosphite oxidation step and an optional capping step. The novel methods improve the quality of synthetic oligonucleotides due to the irreversibility of the front end deprotection step, which prevents the formation of deletion sequences, and due to the avoidance of acidic reagents in the synthesis cycles, which prevent the formation of depurination side products. The invention further discloses novel nucleoside phosphoramidite compositions wherein the phosphoramidites carry acyl front end protective groups which are cleavable with primary amines or phenolates. The invention is applicable to the synthesis of oligodeoxyribonucleotides, oligoribonucleotides and oligonucleotides with modifications in their sugar or phosphate groups.
专利号:US-8299206-B2 优先权日:2007-11-15 标题:Method of synthesis of morpholino oligomers 发明人:FOX CHRISTINA MARY JOSEPHINE; WELLER DWIGHT D 权利人:FOX CHRISTINA MARY JOSEPHINE; WELLER DWIGHT D; AVI BIOPHARMA INC 摘要:Improved methods are described for solid-phase synthesis of morpholino oligomers, in which a protected morpholino ring nitrogen is deprotected between coupling steps using a heterocyclic amine salt in a trifluoroethanol-containing solvent, where the salt is a salt of a heterocyclic amine, having a pKa in the range of 1-4 in its protonated form, with an acid selected from a sulfonic acid, trifluoroacetic acid, and hydrochloric acid. Examples are 3-chloropyridinium methanesulfonate (CPM) and 4-cyanopyridinium trifluoroacetate (CYTFA).
专利号:US-8076476-B2 优先权日:2007-11-15 标 题 :Synthesis of morpholino oligomers using doubly protected guanine morpholino subunits 发明人:REEVES MATTHEW DALE; WELLER DWIGHT D; LI YONGFU 权利人:REEVES MATTHEW DALE; WELLER DWIGHT D; LI YONGFU; AVI BIOPHARMA INC 摘要:Morpholino compounds are provided having the structure: n nwheren R 1 is selected from the group consisting of lower alkyl, di(lower alkyl)amino, and phenyl; R 2 is selected from the group consisting of lower alkyl, monocyclic arylmethyl, and monocyclic (aryloxy)methyl; R 3 is selected from the group consisting of triarylmethyl and hydrogen; and Y is selected from the group consisting of: a protected or unprotected hydroxyl or amino group; a chlorophosphoramidate group; and a phosphorodiamidate linkage to the ring nitrogen of a further morpholino compound or a morpholino oligomer. Such compounds include doubly protected morpholino guanine (MoG) monomers. Also described is their use in synthesis of morpholino oligomers.
专利号:WO-9000622-A1 优先权日:1988-07-08 标题 :Oligonucleotide hybridization probes and means for the synthesis of the most preferred probes 发明人:KWIATKOWSKI MAREK; SUND CHRISTIAN; HURSKAINEN PERTTI 权利人:WALLAC OY; PHARMACIA AB 摘要:Oligonucleotide probe labeled at one of its teminal positions with a non-linear branched polymer carrying a plurality of negatively charged groups, preferably phosphodiester groups, and optionally also analytically indicatable groups covalently linked to terminal ends of the branches of said polymer. The preferred indicatable groups are lanthanide chelates. A compound that can be used for the synthesis of the probe is also disclosed. The compound has formula (I), where R1 and R2 are lower alkyl; R3 is lower alkyl (C1-C7), or aryl each of which optionally being provided with electron-withdrawing substituents; and A1, A2 and A3 are hydrogen, A'-O-B, A''-O-B or A'''-O-B, at most one of A1-3 being hydrogen and A', A'' and A''' being a hydrocarbon chain providing a distance of 5-9 atoms between the phosphorous atom and the oxygen directly bound to B, and B being a protecting group. In the preferred compound at least two of A1-3 are identical while the other is hydrogen.
专利号:EP-1960423-B1 优先权日:2004-12-30 标 题:Synthesis of peptide t-20 using peptide intermediate fragments 发明人:HAN YEUN-KWEI; JOHNSTON DAVID A; KHATRI HIRALAL N 权利人:HOFFMANN LA ROCHE 摘要:Methods for the solid phase synthesis of T-20 peptides and peptide intermediates, in particular methods involving synthesizing T-20 peptide intermediates at low loading factors to produce products having excellent purity and yield.
[参考文献]: A Wissner, Et Al. Analogues Of Platelet Activating Factor. 6. Mono- And Bis-Aryl Phosphate Antagonists Of Platelet Activating Factor. J Med Chem. 1992 May 1;35(9):1650-62.