乙硫醚 反应生成 甲基乙基硫醚 参考文献:Challenger; Rawlings,Journal Of The Chemical Society,1937,P. 872 标题:Challenger; Rawlings,Journal Of The Chemical Society,1937,P. 872
专利号:US-6683189-B1 优先权日:1996-02-26 标 题 :Method for the synthesis of pyrrole and imidazole carboxamides on a solid support 发明人:DERVAN PETER B; BAIRD ELDON 权利人:CALIFORNIA INST OF TECHN 摘要:The present invention describes a novel method for the solid phase synthesis of polyamides containing imidazole and pyrrole carboxamides. The polyamides are prepared on a solid support from aromatic carboxylic acids and aromatic amines with high stepwise coupling yields (>99%), providing milligram quantities of highly pure polyamides. The present invention also describes the synthesis of analogs of the natural products Netropsin and Distamycin A, two antiviral antibiotics. The present invention also describes a novel method for the solid phase synthesis of imidazole and pyrrole carboxamide polyamide-oligonucleotide conjugates. This methodology will greatly increase both the complexity and quantity of minor-groove binding polyamides and minor-groove binding polyamide-oligonucleotide conjugates which can be synthesized and tested.
专利号:WO-9837078-A1 优先权日:1997-02-20 标题 :Solid phase and combinatorial synthesis of substituted thiophenes and of arrays of substituted thiophenes 发明人:DOERWALD FLORENCIO ZARAGOZA 权利人:NOVO NORDISK AS 摘要:A solid phase method for the synthesis of a plurality of differently substituted thiophenes with a wide variety of side-chain substituents as compounds of potential therapeutic interest. The thiophenes are prepared by reaction of a substrate-bound primary or secondary amine with a thiophosgene equivalent and reaction of the resulting intermediate with an acceptor-substituted acetonitrile in the presence of a base. Alkylation with an appropriate alkyl halide, followed by Thorpe-Ziegler-cyclization yields differently substituted, support-bound 3-aminothiophenes. These may be screened on the substrate or cleaved from the substrate and then screened in solution. Alternatively, the resin-bound 3-amino thiophenes or the synthetic intermediates can be subjected to further synthetic transformations (N-acylation, reduction) on the support, which permits the preparation of further therapeutically interesting compounds. The efficient synthesis of a wide variety of thiophenes using automated synthesis technology of the present method makes these compounds attractive candidates for the generation and rapid screening of diverse thiophene-based libraries. The method disclosed here provides an easy and fast access to highly diverse heterocyclic compounds of therapeutic interest, amenable to automatization.
专利号:WO-9740025-A1 优先权日:1996-04-19 标 题 :Solid phase and combinatorial synthesis of substituted 1,2,3-triazoles and of arrays of substituted 1,2,3-triazoles 发明人:DOERWALD FLORENCIO ZARAGOZA 权利人:NOVO NORDISK AS; DOERWALD FLORENCIO ZARAGOZA 摘要:A solid phase method for the synthesis of a plurality of differently substituted 1,2,3-triazoles with a wide variety of side-chain substituents as compounds of potential therapeutic interest. The 1,2,3-triazoles are prepared by acylation of a substrate-bound primary or secondary amine with a 3-oxoalkanoic acid and reaction of the resulting amide with a primary amine under dehydrating conditions to give an enamine. Treatment of this substrate-bound enamine with a sulfonyl azide in the presence of a base gives the corresponding 1,2,3-triazoles. These may be screened on the substrate or cleaved from the substrate and then screened in solution. The efficient synthesis of a wide variety of 1,2,3-triazoles using automated synthesis technology of the present method makes these compounds attractive candidates for the generation and rapid screening of diverse triazole-based libraries. The method disclosed here provides an easy and fast access to highly diverse heterocyclic compounds of therapeutic interest, amenable to automatization.
专利号:US-2024051918-A1 优先权日:2022-08-10 标 题 :Sequential and independent synthesis of mercaptans and asymmetrical sulfides in a single reactor 发明人:LASSEN KENNETH M; NWAGWU UGOCHUKWU; HASENBERG DANIEL M 权利人:CHEVRON PHILLIPS CHEMICAL CO LP 摘要:The present disclosure generally relates to processes to produce a mercaptan and an asymmetrical sulfide utilize stacked bed catalyst systems containing CoMo and NiMo, and these processes demonstrate a synergistic reduction in the amount of ethylene, methyl mercaptan, ethyl mercaptan, and H2S in product mixtures. In aspects, the conversion of limiting reactants in the synthesis of asymmetrical sulfides unexpectedly remain high under increased flow rates through the catalyst bed, and under reduced temperatures and pressures. In further aspects, reactor systems configured for the independent synthesis of mercaptans and asymmetrical sulfides in a single fixed bed catalyst vessel are also disclosed as a simplification of existing reactor systems employing separate reactors for separate mercaptan and sulfide syntheses.
专利号:US-2024217995-A1 优先权日:2021-04-23 标 题 :Compositions for chemical synthesis of peptides 发明人:SEIFERT COLE 权利人:SEDERMA SA 摘要:The disclosure relates to compositions that can serve as anchors for the chemical synthesis of peptides. Anchor molecules can include GAP constituents, linker constituents, amino acid constituents, and/or stopper constituents. Anchor molecules can also include anchor peptides, wherein an anchor peptide can be removably coupled with an amino acid of a given sequence and act as a GAP anchor by achieving solubility control over the target peptide as it is synthesized via the addition of one or more other amino acids: the anchor peptide can then be removed from the target peptide. A novel method of peptide synthesis that utilizes novel anchor molecules and/or anchor peptides is also presented.
专利号:US-2004018598-A1 优先权日:2000-05-30 标题 :Bio-intermediates for use in the chemical synthesis of polyketides 发明人:SANTI DANIEL; ASHLEY GARY; MYLES DAVID C 摘要:The present invention relates to compounds made by a subset of modules from one or more polyketide synthase (“PKSâ€?) genes that are used as starting material in the chemical synthesis of novel molecules, particularly naturally occurring polyketides or derivatives thereof. The biologically derived intermediates (“bio-intermediatesâ€?) generally represent particularly difficult compounds to synthesize using traditional chemical approaches due to one or more stereocenters. In one aspect of the invention, an intermediate in the synthesis of epothilone is provided that feeds into the synthetic protocol of Danishefsky and co-workers. In another aspect of the invention, intermediates in the synthesis of discodermolide are provided that feed into the synthetic protocol of Smith and co-workers. By taking advantage of the inherent stereochemical specificity of biological processes, the syntheses of key intermediates and thus the overall syntheses of compounds like epothilone and discodermolide are greaty simplified.
参考文献:10.1016/s0014-5793(02)02468-7 摘要:Demirhan I, Kanyalkar M, Chandra A, Doerr HW, Coutinho E, Loewer J, Saran A, Chandra P. Docking studies reveal a selective binding of D-penicillamine to the transactivator protein of human immunodeficiency virus type 1. FEBS Lett. 2002 Apr 10;516(1-3):43–6. doi: 10.1016/s0014-5793(02)02468-7. 参考文献:10.1016/j.jasms.2006.07.013 摘要:Amunugama M, Roberts KD, Reid GE. Mechanisms for the selective gas-phase fragmentation reactions of methionine side chain fixed charge sulfonium ion containing peptides. Journal of The American Society for Mass Spectrometry. 2006 Dec 01;17(12):1631–42. doi: 10.1016/j.jasms.2006.07.013.