CAS: 121492-06-6; N-Boc-(2-Aminoethyl)-N-Methylamine

该化合物是有机合成和peptide化学中常用的一种受保护的矿物质衍生物,其主要优势在于三氧碳基(Boc)保护组,该组在多种反应条件下保护主要矿物质功能,同时保持稳定.Boc组可以在温酸条件下有选择地被清除,使该化合物对相继合成战略具有价值.氮的甲基替代会增强消毒控制,减少副作用.这一试剂在复杂分子的准备方面特别有用,因为有选择地取消保护和功能组的兼容性至关重要.其稳定性和多功能性使它在医药化学和生物融合应用中成为首选.

结构式图片

欧盟法规

ECHA物质C&L通报

上下游产品

tert-butyl dicarbonatedi-tert-butyl dicarbonate N-methyl-ethane-1,2-diamine((S)-5-[2-(tert-Butoxycarbonyl-methyl-amino)-ethylcarbamoyl]-5-{(S)-2-[(R)-2-(9H-fluoren-9-ylmethoxycarbonylamino)-propionylamino]-3-phenyl-propionylamino}-pentyl)-carbamic acid 9H-fluoren-9-ylmethyl ester tert-butyl (2-(((benzyloxy)carbonyl)amino)ethyl)(methyl)carbamate {2-[5-[2-(tert-Butoxycarbonyl-methyl-amino)-ethylamino]-7-(4-methoxy-benzyloxy)-6-oxo-6H-1,2,9-triaza-aceanthrylen-2-yl]-ethyl}-(2-hydroxy-ethyl)-carbamic acid tert-butyl ester 2)2-N(Me)-B°CZ-D-Ala-Phe-Lys(Z)-NH-(CH2)2-N(Me)-B°C

合成工艺路线路线简述

  • 合成目标产物 N-Boc-N-Methylethylenediamine 主要起始原料 2-(2-N-Boc-N-Methyl-Aminoethyl)-1H-Isoindole-1,3(2H)-Dione
  • (文献来源)合成步骤主要原料 2-(2-N-Boc-N-Methyl-Aminoethyl)-1H-Isoindole-1,3(2H)-Dione
叔丁氧羰酰基肌氨酸置于ammonium Hydroxide,三乙胺,Diborane(6)体系中,用 四氢呋喃 用作溶剂,化学反应 2.0H,反应生成N-Boc-N-甲基乙二胺
参考文献:脲类肽拟肽的合成方法
标题:脲类肽拟肽的合成方法
摘要:尿素肽类肽模拟物可由boc保护的n-取代的乙二胺组成.最好的方法是由氯乙腈合成这些化合物,然后转化为相应的结晶对硝基苯基氨基甲酸酯,以制备脲类肽.
Doi:10.1016/s0040-4039(97)01166-0

海关参考信息

专利信息


专利号:US-8557979-B2
优先权日:2004-06-10
标题 :Carbapenem antibacterials with gram-negative activity and processes for their preparation
发明人:CHOI WOO-BAEG; KOWALIK EWA
权利人:CHOI WOO-BAEG; KOWALIK EWA; FOB SYNTHESIS INC
摘要:The present invention provides β-methyl carbapenem compounds and pharmaceutical compositions useful in the treatment of bacterial infections and methods for treating such infections using such compounds and/or compositions. The invention includes administering an effective amount of a carbapenem compound or salt and/or prodrug thereof to a host in need of such a treatment. The present invention is also in the field of synthetic organic chemistry and is specifically provides an improved method of synthesis of β-methyl carbapenems which are useful as antibacterial agents.

专利号:US-10933051-B2
优先权日:2017-06-09
标 题 :Carbapenem compounds and compositions for the treatment of bacterial infections
发明人:CHOI WOO-BAEG; TOMIOKA TAKASHI; JOO HYUNG-YEUL; TRUONG PHONG; MIN BRIAN
权利人:FOB SYNTHESIS INC
摘要:The present invention provides carbapenem compounds and pharmaceutical compositions useful in the treatment of bacterial infections, including drug resistant or multiple-drug resistant bacterial infections, and methods for treating such infections using such compounds and/or compositions. The invention includes administering an effective amount of a carbapenem compound or salt and/or prodrug thereof to a host in need of such a treatment.

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-6593347-B2
优先权日:1998-10-30
标题 :Nitrosated and nitrosylated nonsteroidal antiinflammatory compounds, compositions and methods of use
发明人:BANDARAGE UPUL K; DONG QING; FANG XINQIN; GARVEY DAVID S; MERCER GREGORY J; RICHARDSON STEWART K; SCHROEDER JOSEPH D; WANG TIANSHENG
权利人:NITROMED INC
摘要:The present invention describes novel nitrosated and/or nitrosylated nonsteroidal antiinflammatory compounds, and novel compositions comprising at least one nitrosated and/or nitrosylated nonsteroidal antiinflammatory compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase. The present invention also provides methods for treating, preventing and/or reducing inflammation, pain, and fever; decreasing or reversing the gastrointestinal, renal and other toxicities resulting from the use of nonsteroidal antiinflammatory drugs; treating and/or preventing gastrointestinal disorders; treating inflammatory disease states and disorders; and treating and/or preventing ophthalmic diseases or disorders.

专利号:US-10377784-B2
优先权日:2014-03-15
标 题 :Design, synthesis, and biological activity of platinum-benz[c]acridine hybrid agents and methods associated therewith
发明人:BIERBACH ULRICH; PICKARD AMANDA J
权利人:UNIV WAKE FOREST
摘要:The present invention relates to the compounds of formula (I), pharmaceutically acceptable salts, and solvates thereof, wherein the various substituents are as defined herein. The compounds, solvates and salts thereof of Formula (I) are effective as anti-cancer compounds.

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).
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合成参考文献


参考文献:10.1007/s10989-025-10726-x
摘要:Xie Y, Lopez-Silva TL, Dyba MA, Grkovic T, Schneider JP. Elucidation and Prevention of an Unexpected Methylamine Byproduct Formed During Trifluoroacetic Acid-Mediated Side Chain Deprotection of Azido-Containing Peptides. Int J Pept Res Ther. 2025 May 14;31(4). doi: 10.1007/s10989-025-10726-x.
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