ipso-Nitrosation of arylboronic acids with chlorotrimethylsilane and sodium nitrite
摘要:
Nitroso compounds are versatile reagents in synthetic organic chemistry. Herein, we disclose a feasible protocol for the ipso-nitrosation of aryl boronic acids using chlorotrimethylsilane-sodium nitrite unison as nitrosation reagent system. (c) 2014 Elsevier Ltd. All rights reserved.
Direct synthesis of anilines and nitrosobenzenes from phenols
作者:A. H. St. Amant、C. P. Frazier、B. Newmeyer、K. R. Fruehauf、J. Read de Alaniz
DOI:10.1039/c6ob00073h
日期:——
A one-pot synthesis of anilines and nitrosobenzenes from phenols has been developed using an ipso-oxidative aromatic substitution (iSOAr) process. The products are obtained in good yields under mild and metal-free conditions. The leaving group effect on reactions that proceed through mixed quionone monoketals has also been investigated and a predictive model has been established.
已经使用ipso-氧化性芳族取代(i S O Ar)方法开发了一种从苯酚一锅合成苯胺和亚硝基苯的方法。在温和且不含金属的条件下,可以以高收率获得产品。还研究了离去基团对通过混合的醌酮单缩酮进行的反应的影响,并建立了预测模型。
Linker molecule and use thereof in methods for purifying peptides
申请人:BELYNTIC GMBH
公开号:US10954266B2
公开(公告)日:2021-03-23
The present invention relates to a method for the purification of peptides which are produced by solid phase peptide synthesis (SPPS) and corresponding linker molecules for use in said method.
本发明涉及一种通过固相肽合成(SPPS)生产的肽的纯化方法,以及用于所述方法的相应连接分子。
GLP-1 Derivatives and Uses Thereof
申请人:Novo Nordisk A/S
公开号:US20170320927A1
公开(公告)日:2017-11-09
The invention relates to a derivative of a GLP-1 analogue of a general Formula I, which derivative comprises a side chain attached to a Lys residue at position 34, 35, 36, 37, or 38 of the GLP-1 analogue, which side chain comprises a Branched linker, a 1
st
and a 2
nd
Protractor selected from C18 diacid, C20 diacid, and sulfonic acid C16, and at least one Linker element-1 incorporating ethylene glycol units. Linker element-1 may be incorporated in an optional Pre-linker, and/or in a 1
st
or 2
nd
Post-linker. The invention also relates to novel GLP-1 analogues, novel side chain intermediate products and their manufacture and use to prepare derivatives of biologically active peptides and proteins, as well as pharmaceutical compositions and medical uses of the analogues and derivatives. The derivatives have very long half-lives while maintaining a satisfactory potency, which makes them potentially suitable for once-monthly administration.
LINKER MOLECULE AND USE THEREOF IN METHODS FOR PURIFYING PEPTIDES
申请人:BELYNTIC GMBH
公开号:US20190309013A1
公开(公告)日:2019-10-10
The present invention relates to a method for the purification of peptides which are produced by solid phase peptide synthesis (SPPS) and corresponding linker molecules for use in said method.
TRACELESS REDUCTIVELY CLEAVABLE LINKER MOLECULES FOR PEPTIDE PURIFICATION
申请人:BELYNTIC GMBH
公开号:US20210332082A1
公开(公告)日:2021-10-28
The present invention relates to linker molecules of formula (1), X-T
b
-V
a
—U—Y—Z (1) and a method for purifying peptides using said linker molecules. The linker molecule can be coupled to a purification resin via the moiety X and to a peptide via the moiety Y under the release of the leaving group Z. T is an optional spacer moiety and V is an optional electron withdrawing moiety. U is an aryl or 5- or 6-membered heteroaryl moiety bound to at least one electron withdrawing moiety V, W or E. The linker is stable under acidic conditions and releases the peptide upon addition of a reducing agent.