乙基磺酰氯置于sodium Sulfide,碳酸氢钠体系中,用 水 用作溶剂,化学反应 2.0H,以96%的收率获得乙烷亚磺酸钠 参考文献:One-Pot Synthesis Of Symmetric 1,7-Dicarbonyl Compounds Via A Tandem Radical Addition-elimination-addition Reaction 标题:One-Pot Synthesis Of Symmetric 1,7-Dicarbonyl Compounds Via A Tandem Radical Addition-elimination-addition Reaction 摘要:一种新方法已经被开发,通过s-羰基甲基黄嘌呤与环基甲基亚砜及其类似物的串联自由基加成-消除-加成反应合成对称的1,7-二羰基化合物.自由基是通过向s-羰基甲基黄嘌呤中添加二月桂油过氧化物生成的,并与环基甲基亚砜或其类似物反应生成末端烯烃作为中间体.过量的自由基立即与中间烯烃反应,形成对称的1,7-二羰基化合物的加合物.这是一种在温和条件下合成1,7-二羰基化合物的高效方法. Doi:10.1039/c3Ra42932F
专利号:US-7329515-B2 优先权日:2003-04-21 标题 :Solid support for the synthesis of 3′-amino oligonucleotides 发明人:LEUCK MICHAEL; WOLTER ANDREAS 权利人:SIGMA ALDRICH CO 摘要:The present invention discloses novel methods and solid supports for the synthesis of 3′-amino oligonucleotides. The novel supports are based on an unsubstituted or ring-substituted hydroxymethylbenzoyl linker element wherein the hydroxymethyl group is esterified to a solid phase bound carboxylic acid and the carbonyl group is linked to an amino alcohol as an amide. Oligonucleotides are conveniently synthesized on the novel supports with no modifications in the standard phosphoramidite synthesis scheme. The ester function of the support is cleaved under the alkaline deprotection conditions for oligonucleotides to provide a free hydroxymethyl group that aids in the release of the 3′-amino oligonucleotide products with a free amino group through neighbor group participation. The free amino group of the oligonucleotides is available for further conjugation reactions to haptens, reporter groups, surfaces or other small molecules or biomolecules. The methods provided are particularly mild, do not require any modifications in standard protocols for the synthesis and deprotection of oligonucleotides, provide the 3′-amino oligonucleotides free of side products and do not introduce chiral centers to the oligonucleotides.
专利号:US-7429658-B2 优先权日:2003-09-11 标题 :Synthesis of protected pyrrolobenzodiazepines 发明人:HOWARD PHILIP; MASTERSON LUKE 权利人:SPIROGEN LTD 摘要:A method of synthesis of a N-10 protected PBD compound of formula (I): n nvia an intermediate of formula (II) or formula (V):
专利号:US-7329760-B2 优先权日:2002-04-05 标题 :CC-1065 analog synthesis 发明人:ZHAO ROBERT YONGXIN; CHARI RAVI V J 权利人:IMMUNOGEN INC 摘要:Improved synthesis of seco(−)CBI (5-hydroxy-3-amino-1-[S]-(chloromethyl)-1,2-dihydro-3H-benz(e)indole): n nand improved syntheses therefrom of a wide variety of CC-1065 analogs that comprise a cyclopropabenzidole (CBI) alkylating moiety, and which are collectively DC1 and its derivatives, for the synthesis of cell-targeted therapeutic agents.
专利号:US-7288120-B2 优先权日:2003-12-12 标题 :Synthesis of tetraazapentamethine compounds, and processes for dyeing keratin fibers using this synthesis 发明人:PEREIRA RUI; BURGAUD HERVE 权利人:OREAL 摘要:The present disclosure relates to processes for synthesizing tetraazapentamethine compounds that comprise reacting at least one compound of azine type with at least one oxidizing agent. The disclosure also relates to processes for dyeing keratin fibers, for example human keratin fibers, that comprise using such synthetic processes.
专利号:US-7038037-B2 优先权日:2002-06-20 标题 :Method for sequential support-bound synthesis of conjugated oligomeric compounds 发明人:MAIER MARTIN A; GUZAEV ANDREI P; MANOHARAN MUTHIAH 权利人:ISIS PHARMACEUTICALS INC 摘要:A sequential support-bound synthesis method is disclosed for preparing a conjugated oligomeric compound, preferably a PNA-peptide conjugate or an oligonucleotide-peptide conjugate, using a bridging molecule having at least two N-protecting amino groups. A conjugated oligomeric compound for therapeutic or prophylactic delivery is also disclosed.
专利号:WO-2005100378-A1 优先权日:2004-04-13 标 题:Process for the preparation of a peptide, and compounds comprising a thioester carboxyl-activating group for use therein 发明人:EVANS DAVID JOHN 权利人:AVECIA LTD; EVANS DAVID JOHN 摘要:There is provided a process for the solid-phase synthesis of a polymer which comprises reacting an amine, secondary amine or hydroxyl group of a first monomer with a thioester on a second monomer wherein at least one the monomers is immobilised on a solid-phase support. There is also provide novel activated amino acids of Formula (1) wherein: R is an amino acid side chain a protected amino acid side chain or a peptide chain; X is an amino protecting group; and Z is an optionally substituted hydrocarbyl, and certain supported activated amino acids of Formula (5) wherein: SUPPORT is a solid support; L is a linking group; R is an amino acid side chain; a protected amino acid side chain or a peptide chain; and X3is an amino protecting group or one or more amino acids linked by amide bonds where the terminal residue bears an amino protecting group for use in said process.