三甲基乙酸乙酯置于lithium Aluminium Tetrahydride体系中,化学反应生成2-(三甲硅基)乙醇 参考文献:The Addition Of Silicon Hydrides To Olefinic Double Bonds. Part Ii. The Use Of Group Viii Metal Catalysts 标题:The Addition Of Silicon Hydrides To Olefinic Double Bonds. Part Ii. The Use Of Group Viii Metal Catalysts 摘要: Doi:10.1021/ja01561A054
专利信息
专利号:WO-2010103857-A1 优先权日:2009-03-12 标 题 :Method for solid-phase synthesis of glycopeptide using silicon-containing protecting group and synthesis device 发明人:NISHIMURA SHIN-ICHIRO; SHIMAWAKI KEN 权利人:UNIV HOKKAIDO NAT UNIV CORP; NISHIMURA SHIN-ICHIRO; SHIMAWAKI KEN 摘要:Disclosed are a novel method for the synthesis of a glycopeptide by which glycopeptides of various types can be deprotected and excised from a resin, each under weakly acidic to weakly basic conditions, without causing the problems of the epimerization of an amino acid at the a-position and the ß-elimination of a sugar residue; a synthesis device therefor; and a synthesis intermediate to be used in synthesizing a glycopeptide. Specifically disclosed are a method for the solid-phase synthesis of a glycopeptide which comprises a step for obtaining a glycopeptide derivative wherein the N-terminus is protected, the C-terminus is immobilized to a solid phase via a silicon linker, and a reactive group carried by a sugar residue and a reactive group carried by an amino acid side chain constituting a peptide are protected by silicon-containing groups, and a step for obtaining the glycopeptide by deprotecting said glycopeptide derivative and releasing the same from the solid phase by treating the glycopeptide derivative with an agent for removing the silicon-containing groups and the silicon linker; a synthesis intermediate to be used in the step for obtaining the glycopeptide derivative in the aforesaid method; and a device for the solid-phase synthesis of a glycopeptide.
专利号:US-2004242897-A1 优先权日:2002-07-31 标题 :Universal support media for synthesis of oligomeric compounds 发明人:GUZAEV ANDREI P; MANOHARAN MUTHIAH 摘要:Compounds for the synthesis of oligomeric compounds, particularly oligonucleotides and oligonucleotide mimetics, are provided. In addition, methods for functionalizing a support medium with a first monomeric subunit and methods for the synthesis of oligomeric compounds utilizing the novel compounds bound to support media are provided.
专利号:US-6063919-A 优先权日:1998-08-14 标题:Process for the synthesis of exochelins 发明人:GAUDIOSO LARRY A; WEGLARZ MICHAEL A 权利人:KEYSTONE BIOMEDICAL INC 摘要:A process for the synthesis of an Exochelin comprising the steps of generating L-N-[(2-benzyloxy-(benzoyl)] serine or L-N-[2-benzyloxy (benzoyl)] threonine, creating L-N-t-Boc- epsilon -hydroxynorleucine and reacting same to produce L-N-Boc- epsilon -bromonorleucine trimethylsilylethyl ester, providing a dicarboxylic acid and forming an O-benzyl methyl hydroxamate from the dicarboxylic acid, coupling the O-benzyl methyl hydroxamate with the L-N-Boc- epsilon -bromonorleucine trimethylsilylethyl ester to give an L-N2-Boc-N6-methyl,N6-(benzyloxy) lysine 2-trimethylsilylethyl ester which incorporates the dicarboxylic acid as modified above, removing the N-tert-butoxycarbonyl protecting group from the L-N2-Boc-N6-methyl, N6-(benzyloxy) lysine 2-trimethylsilylethyl ester to yield a substituted lysine, and coupling the same with the L-N-[2-benzyloxy (benzoyl) serine or -threonine to yield a 2-trimethyl silylethyl ester of dibenzyl Exochelic acid, transforming the 2-trimethyl silylethyl ester of dibenzyl Exochelic acid to dibenzyl Exochelic acid, preparing benzyl epi-cobactin, forming an ester bond between the dibenzyl Exochelic acid and benzyl epi-cobactin to form an intermediate, and, hydrogenolytically removing three benzyl groups from said intermediate, resulting in the synthesized Exochelin. More particularly, a synthesis for Exochelin 786SM (R) is disclosed wherein the dicarboxylic acid is suberic acid and the serine form is utilized.
专利号:WO-2004011474-A1 优先权日:2002-07-31 标题:Universal support media for synthesis of oligomeric compounds 发明人:GUZAEV ANDREI P; MANOHARAN MUTHIAH; RAVIKUMAR VASULINGA T; KUMAR RAJU K 权利人:ISIS PHARMACEUTICALS INC; GUZAEV ANDREI P; MANOHARAN MUTHIAH; RAVIKUMAR VASULINGA T; KUMAR RAJU K 摘要:Compounds for the synthesis of oligomeric compounds, particularly oligonucleotide and oligonucleotide mimetics, are provided. In addition, methods for functionalizing a support medium with a first monomeric subunit and methods for the synthesis of oligomeric compounds utilizing the novel compounds bound to support media are provided.
专利号:WO-2017033128-A1 优先权日:2015-08-25 标题 :Biphenyl-substitued 4-amino-butyric acid derivatives and their use in the synthesis of nep inhibitors 发明人:HOOK DAVID; KU JIE; ZHOU JIANGUANG 权利人:NOVARTIS AG; HOOK DAVID; KU JIE; ZHOU JIANGUANG 摘要:The invention relates to a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, in particular neutral endopeptidase (NEP) inhibitors and prodrugs thereof.
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):
参考标题:Alkyl 1-Chloroalkyl Carbonates: Reagents For The Synthesis Of Carbamates And Protection Of Amino Groups 作者:Gérard Barcelo,Jean-Pierre Senet,Gérard Sennyey,Jean Bensoam,Albert Loffet 摘要:The Synthesis Of 1-Chloroalkyl Carbonates And Their Reaction With Various Type Of Amines Are Described. This Reaction Is Useful For The Synthesis Of Carbamate Pesticides And For The Protection Of Various Amino Groups, Including Amino Acids.
合成参考文献
摘要:Joule, J. A., Science of Synthesis Knowledge Updates, (2010) 2, 374. 摘要:Joule, J. A., Science of Synthesis Knowledge Updates, (2010) 2, 405. 摘要:Johnson, J. B., Science of Synthesis: Stereoselective Synthesis, (2011) 3, 778. 摘要:de Frémont, P., Science of Synthesis: N-Heterocyclic Carbenes in Catalytic Organic Synthesis, (2016) 1, 404. 摘要:Shao, Z.; Deng, Y.-H., Science of Synthesis, (2019) , 3.