专利号:US-9884885-B2 优先权日:2009-05-18 标题:Synthesis of labile base protected-modified deoxy and modified ribo nucleosides, corresponding phosphoramidites and supports and their use in high purity oligonucleotide synthesis 发明人:SRIVASTAVA SURESH C; SRIVASTAVA NAVEEN P 权利人:SRIVASTAVA SURESH C; SRIVASTAVA NAVEEN P; CHEMGENES CORP 摘要:This invention relates to novel method of synthesis of RNA utilizing N-2-acetyl protected guanine as nucleoside base, nucleosides, succinates, phosphoramidites, corresponding solid supports that are suitable for oligo deoxy nucleosides and RNA oligonucleotide synthesis. Our discovery using N-acetyl protected guanine as nucleoside base protecting group, which is significantly faster base labile protecting group, yet significantly more stable than commonly utilized-2-isobutyryl guanosine is a novel approach to obtain highest purity oligonucleotides. This approach is designed to lead to very high purity and very clean oligonucleotide, after efficient removal of the protecting groups, including acetyl group from guanine and to produce high purity therapeutic grade DNA oligonucleotides, RNA oligonucleotides, diagnostic DNA, diagnostic RNA for microarray platform. The deprotection of acetyl protecting groups of the natural deoxy and ribonucleosides occurs under substantially reduced time in contact with mild deprotection conditions such as mild bases, secondary amines for removal of such groups under such conditions would allows synthesis of various DNA and RNA of highest purity for diagnostics and therapeutic application. This approach is designed to lead to high purity large scale therapeutic grade oligonucleotide chimeras which consist of fluoro sugar modification in conjunction with deoxy nucleosides, ribonucleosides, modified base and modified sugar nucleosides. This approach is further designed to use acetyl guanine protecting group when other bases are sensitive nucleoside, and for use in oligo peptide synthesis and for support bound oligo nucleotides.
专利号:US-7652164-B2 优先权日:2005-09-13 标题:Process for the direct synthesis of trialkoxysilane 发明人:LEWIS KENRICK M; MEREIGH ABELLARD T; O'YOUNG CHI-LIN; CAMERON RUDOLPH A 权利人:MOMENTIVE PERFORMANCE MAT INC 摘要:The Direct Synthesis of trialkoxysilane is carried out by conducting the Direct Synthesis reaction of silicon and alcohol, optionally in solvent, in the presence of a catalytically effective amount of Direct Synthesis catalyst and an effective catalyst-promoting amount of Direct Synthesis catalyst promoter, said promoter being an organic or inorganic compound possessing at least one phosphorus-oxygen bond.
专利号:US-9353057-B2 优先权日:2003-12-30 标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof 发明人:GALLOP MARK A; DAI XUEDONG; SCHEUERMAN RANDALL A; RAILLARD STEPHEN P; MANTHATI SURESH K; YAO FENMEI; PHAN THU; LUDWIKOW MARIA; PENG GE; BHAT SEEMA 权利人:XENOPORT INC 摘要:Methods for synthesis of 1-(acyloxy)-alkyl carbamates, particularly, the synthesis of 1-(acyloxy)-alkyl carbamate prodrugs of primary or secondary amine-containing drugs are described. Also described are methods for synthesis of 1-(acyloxy)-alkyl N-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described.
专利号:US-2013267680-A1 优先权日:2010-09-15 标题:Total chemical synthesis of ubiquitin, ubiquitin mutants and derivatives thereof 发明人:OVAA HUIB; EL OUALID FARID; MERKX REMCO NICOLAAS SEBASTIAAN MICHEL 权利人:OVAA HUIB; EL OUALID FARID; MERKX REMCO NICOLAAS SEBASTIAAN MICHEL; STICHTING HET NL KANKERINST 摘要:The present invention relates to the field of total chemical synthesis of ubiquitin and related peptides. More in particular, a method is provided of solid phase synthesis of ubiquitin, ubiquitin mutants and derivatives thereof. It was the object of the present invention to provide an approach for the total chemical synthesis of ubuiqitin, which allows for the chemical synthesis of virtually any Ub mutant and giving high overall efficiency and purity. The present inventors have surprisingly found that this object can be realized with a method relying on incorporation of special amino acid building blocks. This approach was found to allow for exceptionally high yields of up to 14% and to provide an synthetic entry into virtually any ubiquitin derivative.
专利号:US-3992413-A 优先权日:1975-07-25 标 题 :Intermediates in the synthesis of prostaglandins 发明人:TAUB DAVID; WENDLER NORMAN L 权利人:MERCK & CO INC 摘要:The invention relates to a new and novel synthesis of prostaglandin E 2 , and it particularly relates to a novel process starting with relatively inexpensive starting materials. The invention further relates to a synthesis which is readily adaptable for large scale processing because of the high yields in the individual reaction steps. n The invention further relates to novel compounds formed as intermediates in the synthesis of prostaglandin E 2 . The invention still further relates to synthetic analogs and known metabolites of prostaglandin E 2 and prostaglandin E 1 , useful as standards in certain biological assays for determining prostaglandin-like activity.
专利号:US-2010099894-A1 优先权日:2006-10-09 标 题 :Method for the Synthesis of Cyclic Acetals by the Reactive Extraction of a Polyol in a Concentrated Solution 发明人:DUBOIS JEAN-LUC; IBORRA CHORNET SARA; VELTY ALEXANDRA I LUCIENNE; CORMA CANOS AVELINO 权利人:DUBOIS JEAN-LUC; IBORRA CHORNET SARA; VELTY ALEXANDRA I LUCIENNE; CORMA CANOS AVELINO 摘要:A method for the synthesis of cyclic acetals comprises reacting at least one carbonyl-function compound selected from aldehydes, ketones, and/or linear acetals, on a polyol in a concentrated aqueous solution exceeding 20 wt % in a reactor containing an acidic catalyst. The carbonyl-function compound is selected so that the cyclic acetal obtained has a water solubility lower than 20000 mg/kg. During the catalytic reaction for the cyclic acetal synthesis, at least one portion of the organic phase containing the cyclic acetal is separated. The acidic catalysis is either homogeneous when using a water-soluble strong acid, or heterogeneous when using a solid acid such as a resin, a zeolite, or any appropriately acidified solid. The extractive reaction method can be used for obtaining high conversions and selectivity.
参考文献:10.1021/ol201620g 摘要:Jin W, Du W, Yang Q, Yu H, Chen J, Yu Z. Regio- and stereoselective synthesis of multisubstituted olefins and conjugate dienes by using α-oxo ketene dithioacetals as the building blocks. Org Lett. 2011 Aug 19;13(16):4272–5. doi: 10.1021/ol201620g. 参考文献:10.1021/ol201519a 摘要:Petrová M, Buděšínský M, Zborníkovš E, Fiedler P, Rosenberg I. A Ferrier-type allylic rearrangement of 3'-deoxy-3',4'-didehydronucleosides mediated by DMF dimethyl acetal: direct access to 4'-alkoxy-2',3'-didehydro-2',3'-dideoxynucleosides. Org Lett. 2011 Aug 19;13(16):4200–3. doi: 10.1021/ol201519a. 参考文献:10.1021/ja205174c 摘要:Vo CV, Mitchell TA, Bode JW. Expanded substrate scope and improved reactivity of ether-forming cross-coupling reactions of organotrifluoroborates and acetals. J Am Chem Soc. 2011 Sep 07;133(35):14082–9.