N-[(3-Methyl-2-Butenyl)Oxycarbonyl]-2-(1-Cyclohexenyl)Ethylamine置于碘,锌体系中,用 甲醇 用作溶剂,化学反应 7.5H,以88%的收率获得2-(1-环己烯基)乙胺 参考文献:One-Pot Selective Cleavage Of Prenyl Carbamates Using Iodine In Methanol Followed By Zinc 标题:One-Pot Selective Cleavage Of Prenyl Carbamates Using Iodine In Methanol Followed By Zinc 摘要:The Prenyloxycarbonyl (Preoc) Moiety Was Efficiently Removed From Carbamates To Provide The Corresponding Amines In Good To Excellent Yields (63-88%) By Using Iodine In Methanol Followed By Treatment Of The Resulting Beta-Methoxyiodides By Zinc Powder. The Reaction Conditions Are Compatible With The Presence Of A Number Of Functional Groups Such As Boc And Cbz Carbamates,Sulfides,Double Bonds,Indoles And Aromatic Methyl Ethers. (C) 2003 Elsevier Ltd. All Rights Reserved. Doi:10.1016/j.Tetlet.2003.10.058
专利号:US-11161827-B2 优先权日:2019-04-05 标 题 :Catalytic systems for stereoselective synthesis of chiral amines by enantiodivergent radical C—H amination 发明人:Zhang xiao-xiang; Lang kai 权利人:TRUSTEES BOSTON COLLEGE; THE TRUSTEES OF BOSTON COLLEGE 摘要:In one aspect, the disclosure relates to a mode of asymmetric induction in radical processes based on sequential combination of enantiodifferentiative H-atom abstraction and stereoretentive radical substitution. Also disclosed is an asymmetric system for stereoselective synthesis of strained 5-membered cyclic sulfamides via radical 1,5-C—H amination of sulfamoyl azides. The disclosed metalloradical system can control the degree and sense of asymmetric induction in the catalytic radical C—H amination in a systematic manner. The disclosed system is applicable to a broad scope of substrates with different types of C(sp 3 )—H bonds and exhibits reactivity and selectivity, providing access to both enantiomers of useful 5-membered cyclic sulfamides in a highly enantioenriched form. Also disclosed are catalysts useful in these processes. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present disclosure.
专利号:US-5877278-A 优先权日:1992-09-24 标题:Synthesis of N-substituted oligomers 发明人:ZUCKERMANN RONALD N; GOFF DANE A; NG SIMON; SPEAR KERRY; SCOTT BARBARA O; SIGMUND AARON C; GOLDSMITH RICHARD A; MARLOWE CHARLES K; PEI YAZHONG; RICHTER LUTZ; SIMON REYNA 权利人:CHIRON CORP 摘要:A solid-phase method for the synthesis of N-substituted oligomers, such as poly (N-substituted glycines) (referred to herein as poly NSGs) is used to obtain oligomers, such as poly NSGs of potential therapeutic interest which poly NSGs can have a wide variety of side-chain substituents. Each N-substituted glycine monomer is assembled from two 'sub-monomers' directly on the solid support. Each cycle of monomer addition consists of two steps: (1) acylation of a secondary amine bound to the support with an acylating agent comprising a leaving group capable of nucleophilic displacement by -NH2, such as a haloacetic acid, and (2) introduction of the side-chain by nucleophilic displacement of the leaving group, such as halogen (as a solid support-bound alpha -haloacetamide) with a sufficient amount of a second sub-monomer comprising an -NH2 group, such as a primary amine, alkoxyamine, semicarbazide, acyl hydrazide, carbazate or the like. Repetition of the two step cycle of acylation and displacement gives the desired oligomers. The efficient synthesis of a wide variety of oligomeric NSGs using automated synthesis technology of the present method makes these oligomers attractive candidates for the generation and rapid screening of diverse peptidomimetic libraries. The oligomers of the invention, such as N-substituted glycines (i.e. poly NSGs) disclosed here provide a new class of peptide-like compounds not found in nature, but which are synthetically accessible and have been shown to possess significant biological activity and proteolytic stability. Combinatorial libraries of cyclic compounds are disclosed wherein the cyclic compounds are comprised of at least one ring structure derived from cyclization of a peptoid backbone. The diversity of product compounds is generated by the sequential addition of substituted submonomers. The combinatorial library includes 10 or more, preferably 100 or more, and more preferably 1,000 or more distinct and different compounds. The library includes each of the product compounds in retrievable and analyzable amounts and preferably includes at least one biologically active compound. Methods of synthesizing the combinatorial libraries and assay devices produced using the libraries are disclosed as is methodology for screening for and obtaining biologically active cyclic organic compounds.
专利号:US-8148527-B1 优先权日:2011-01-18 标 题:Resolution of 1-(4-methoxybenzyl)-octahydro-isoquinoline 发明人:DIVI MURALI KRISHNA PRASAD; PENDYALA SRINIVAS RAO; RAMANA LAVU VENKATA 权利人:DIVI MURALI KRISHNA PRASAD; PENDYALA SRINIVAS RAO; RAMANA LAVU VENKATA; DIVIS LAB LTD 摘要:The resolution of racemic 1-(4-methoxybenzyl)-octahydro-isoquinoline, a key intermediate in the synthesis of the antitussive agent dextromethorphan, is reported using (R)-2-(6-methoxy-2-naphthyl) propionic acid in good yields. The resolving agent and the undesired isomer of the octahydro-isoquinoline have been recovered in good yield.
专利号:US-8653223-B2 优先权日:2008-04-16 标题:Transketalized compositions, synthesis, and applications 发明人:SELIFONOV SERGEY; GOETZ ADAM EDWARD; JING FENG 权利人:SELIFONOV SERGEY; GOETZ ADAM EDWARD; JING FENG; SEGETIS INC 摘要:Ketal compounds of the structure I n nand a method of preparation of the compound from polyols and oxocarboxylates, as well as uses thereof.
专利号:US-6797820-B2 优先权日:1999-12-17 标 题:Succinate compounds, compositions and methods of use and preparation 发明人:PATEL DINESH; JACOBS JEFFREY W; JAIN RAKESH; NI ZHI-JIE; YUAN ZHENGYU 权利人:VICURON PHARM INC 摘要:Novel hydroxamic acid compounds are disclosed. These hydroxamates inhibit peptidyl deformylase (PDF), an enzyme present in prokaryotes. The hydroxymates are useful as antimicrobials and antibiotics. The compounds of the invention display selective inhibition of peptidyl deformylase versus other metalloproteinases such as matrix metalloproteinases (MMPs). Methods of synthesis and of use of the compounds are also disclosed.
专利号:US-10458995-B2 优先权日:2016-03-25 标 题 :Combinatorial synthesis and biomarker development 发明人:MOOLA MURALIDHAR REDDY 权利人:MOOLA MURALIDHAR REDDY 摘要:Provided herein are methods, kits, and compositions for use in the diagnosis and treatment of diseases. Peptoids recognized by Alzheimers disease specific antibodies are identified.