2-氯乙基甲基醚置于氨体系中,用 甲醇 用作溶剂,化学反应生成双(2-甲氧基乙基)胺 参考文献:Remizov,A.L.,Journal Of General Chemistry Of The Ussr,1964,Vol. 34,# 10,P. 3233-3237 标题:Remizov,A.L.,Journal Of General Chemistry Of The Ussr,1964,Vol. 34,# 10,P. 3233-3237
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-6653087-B1 优先权日:1997-02-07 标 题 :Convergent synthesis of combinatorial library 发明人:BOGER DALE L 权利人:SCRIPPS RESEARCH INST 摘要:Targeted C2-symmetric and unsymmetric chemical libraries for use in protein and receptor homodimerization and heterodimerization are constructed by solution phase methodologies. Exemplary libraries are prepared in a 60 to 10 sub-library format by symmetrical coupling of the constructed fragments with a mixture of tethering dicarboxylic acids. In each step of the 3-step reaction sequence, the reactants, unreacted starting material, reagents and their byproducts were removed by simple liquid-liquid or liquid-solid extractions providing the desired intermediates and final libraries in multi-milligram quantities in high purities (≧90-100%) independent of the reaction yields and without deliberate reaction optimization. The synthesis of a second prototypical library employed the olefin metathesis reaction to join and combinatorially randomize the length of linker tether. This approach provides a unique opportunity to rapidly generate a statistically controlled mixture of homo and heterodimers of remarkable diversity.
专利号:US-6987186-B2 优先权日:2003-01-28 标 题 :Synthesis of small particle size quinacridone of beta crystal phase 发明人:COLE DAMIEN THURBER; JEGANATHAN SURULIAPPA GOWDER; HE YINGXIA 权利人:CIBA SC HOLDING AG 摘要:The present invention relates to a process for the synthesis of beta-quinacridone by oxidation in the presence of selected additives that promote the formation of the desired crystal phase and particle size.
专利号:US-6861531-B2 优先权日:2002-03-27 标 题:Synthesis of 2,6-dicarbonylpyridines 发明人:GATELY DANIEL A 权利人:BOULDER SCIENT CO 摘要:Synthesis of 2,6-dicarbonylpyridines in solution in a hydrocarbon medium is described. The solutions of 2,6-dicarbonylpyridines may be used directly in further syntheses.
专利号:US-2025129021-A1 优先权日:2023-09-19 标 题:Small molecule protein synthesis modulators 发明人:GYGI DAVID; BAHMANYAR SOGOLE SAMI; HAMANN LAWRENCE 权利人:INTERDICT BIO INC 摘要:The present disclosure provides compounds of the formulae herein (e.g., Formula (I), Formula (V)), and pharmaceutically acceptable salts thereof, which are useful for modulating protein synthesis (e.g., modulating synthesis of BCL-2, MYC, CCND1, MCL-1, ALK, KRAS-G12D). The present disclosure also provides pharmaceutical compositions and kits comprising the compounds, or pharmaceutically acceptable salts thereof, and methods of treating or preventing diseases or disorders (e.g., diseases or disorders associated with BCL-2, MYC, CCND1, MCL-1, ALK, KRAS-G12D) by administering to a subject in need thereof the compounds, or pharmaceutically acceptable salts thereof, or pharmaceutical compositions thereof.
专利号:US-6906046-B2 优先权日:2000-12-22 标题 :Pharmaceutical uses and synthesis of benzobicyclooctanes 发明人:JACKSON RANDY W; DARWISH IHAB; BAUGHMAN TED A; HOWBERT J JEFFRY 权利人:CELLTECH R & D INC 摘要:Benzobicyclooctane compounds, their use in inhibiting cellular events involving TNF-α and IL-8, and in the treatment of inflammation events in general; a combinatorial library of diverse bicyclooctanes and process for their synthesis as a library and as individual compounds.
摘要:Sato, N., Science of Synthesis Knowledge Updates, (2011) 4, 316. 摘要:Tomás-Gamasa, M., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 2, 27. 摘要:Fogel, M. S.; Shellnutt, Z. S.; Koide, K., Science of Synthesis: Dearomatizations, (2026) .