N-Boc-脒三苯基膦置于limcpba,Lithium Hexamethyldisilazane体系中,用 四氢呋喃,二氯甲烷,甲苯 用作溶剂,化学反应 20.0H,反应生成Boc-甘氨酸叔-丁基酯 参考文献:N-Alkyloxycarbonyl-3-Aryloxaziridines: Their Preparation,Structure,And Utilization As Electrophilic Amination Reagents 标题:N-Alkyloxycarbonyl-3-Aryloxaziridines: Their Preparation,Structure,And Utilization As Electrophilic Amination Reagents 摘要:Abstractthis Paper Reports The Synthesis Of A Series Of N‐protected Oxaziridines (N‐m°C,B°C,Z Or Fmoc) And Discusses Their Ability To Deliver Their N‐alkoxycar‐bonyl Fragment To Amines,Enolates,Sulfur,And Phosphorus Nucleophiles (Electrophilic Amination). These Oxaziridines Are Prepared By Oxidation Of The Corresponding Imines With Oxone Or Anhydrous Mcpba Lithium Salt As The Source Of Oxygen. They Transfer Their N‐protected Fragment To Primary And Secondary Amines To Give Protected Hydrazines In Fair To Excellent Yield. The Nitrogen Transfer To Free Amino Acids (In Form Of Their R4N+ Salts) Is Particularly Fast,Even At Low Temperature,Providing L (Or D) N‐protected α‐hydrazino Acids. Enolates Are C‐aminated To Give N‐protected α‐amino Ketones,Esters,Or Amides In Modest Yield,Due To A Side Aldol Reaction Of The Unreacted Enolate With The Released Benzaldehyde. With Tertiary Amines (Et3N),Sulfides (Phsme),And Phosphines (Ph3P),Amination And Oxidation Proceed In A Parallel Way; The Amount Of Amination Product Increases When The Temperature Is Lowered (Kinetic Control). Some Of The Factors That Can Orient The Oxaziridine Reactivity Towards Amination Or Oxidation Of Nucleophiles Are Considered. Doi:10.1002/chem.19970031019
专利号:US-2004110228-A1 优先权日:2002-04-01 标 题:Combinatorial organic synthesis of unique biologically active compounds 发明人:MCALPINE SHELLI R; TAYLOR RACHEL E; BOLLA MEGAN L; SEGALL ANCA M 摘要:The invention provides a method for making a combinatorial library of cyclic compounds, such as Holliday junction-trapping compounds, comprising the steps of (a) obtaining a plurality of trimers according to the generic structure X 1- X 2- X 3 , wherein X 1 , X 2 and X 3 can be independently any naturally or nonnaturally occurring amino acids or peptidomimetics thereof; (b) optionally coupling a spacer S to the trimer at either end; (c) cyclizing two trimers or trimer-spacer conjugates in a head-to-tail orientation; thereby obtaining a combinatorial library of compounds, wherein the library does not include an unmodifed or naturally occurring Holliday Junction-trapping compounds. The invention additionally provides methods macrocyclic compounds that are synergimycin derivatives.
专利号:US-9718807-B2 优先权日:2012-06-05 标 题 :Synthesis of antiviral compound 发明人:SCOTT ROBERT WILLIAM; VITALE JUSTIN PHILIP; MATTHEWS KENNETH STANLEY; TERESK MARTIN GERALD; FORMELLA ALEXANDRA; EVANS JARED WAYNE 权利人:GILEAD PHARMASSET LLC 摘要:The present disclosure provides processes for the preparation of a compound of formula I: n nwhich is useful as an antiviral agent. The disclosure also provides compounds that are synthetic intermediates to compounds of formula I.
专利号:US-2023151034-A1 优先权日:2020-03-17 标题:Peptidomimetic n5-methyl-n2-(nonanoyl-l-leucyl)-l-glutaminate derivatives, triazaspiro[4.14]nonadecane derivatives and similar compounds as inhibitors of norovirus and coronavirus replication 发明人:JACOBSON IRINA C; LEE SAM SK; PIZARRO NOVOA JUAN CARLOS 权利人:COCRYSTAL PHARMA INC 摘要:Peptidomimetic N5-methyl-N2-(nonanoyl-L-leucyl)-L-glutaminate derivatives, triazaspiro[4.14]nonadecane derivatives and similar compounds for use in methods of inhibiting the replication of noroviruses and coronaviruses in a biological sample or patient, for use in reducing the amount of noroviruses or coronaviruses in a biological sample or patient, and for use in treating norovirus and coronavirus in a patient, comprising administering to said biological sample or patient a safe and effective amount of a compound represented by formulae I or II, or a pharmaceutically acceptable salt thereof. The present description discloses the synthesis and characterisation of exemplary compounds as well as pharmacological data thereof (e.g. page 99 to page 271; examples 1 to 3; compounds A1 to A104 and B1 to B66; tables A to E).
专利号:US-2005042149-A1 优先权日:1994-04-01 标 题 :Nanoscale chemical synthesis 发明人:BARD ALLEN J 权利人:INTEGRATED CHEMICAL SYNTHESIZE 摘要:A modular reactor system and method for synthesizing nanoscale quantities of chemical compounds characterized by a continuous flow reactor under high pressure having uniform temperature throughout the reaction mixture. The apparatus includes a number of generic components such as pumps, flow channels, manifolds, flow restrictors, valves and at least one modular reactor, as small as one nanoliter in volume, where larger quantities can be produced by either using larger nanoscale sized units or adding parallel and serially disposed nanoscale reactor units.
专利号:US-6828143-B1 优先权日:1994-04-01 标题:Nanoscale chemical synthesis 发明人:BARD ALLEN J 权利人:INTEGRATED CHEMICAL SYNTHESIZE 摘要:A modular reactor system and method for synthesizing nanoscale quantities of chemical compounds characterized by a continuous flow reactor under high pressure having uniform temperature throughout the reaction mixture. The apparatus includes a number of generic components such as pumps, flow channels, manifolds, flow restrictors, valves and at least one modular reactor, as small as one nanoliter in volume, where larger quantities can be produced by either using larger nanoscale sized units or adding parallel and serially disposed nanoscale reactor units.
专利号:US-2013324740-A1 优先权日:2012-06-05 标题:Synthesis of antiviral compound