65833-14-9

Upstream product

• 72000-67-0 3-bromo-1-phenyl-1H-pyrrole-2,5-dione 
• 635-90-5 1-phenylpyrrole 
• 7726-95-6 bromine 
• 64-19-7 acetic acid 
• 181944-34-3 2-nitro-1-phenyl-pyrrole 
• 941-69-5 N-phenyl-maleimide 
• 608-37-7 dibromomaleic acid 
• 62-53-3 aniline 
• 1442447-48-4 3,4-dibromo-2,5-dioxo-2,5-dihydro-pyrrole-1-carboxylic acid methyl ester 
• 58879-90-6 3,4-dibromo-1-phenylpyrrolidine-2,5-dione 
• 1122-12-9 2,3-dibromomaleic anhydride 

Downstream Products

• 15051-40-8 3,4-diiodo-2,5-dihydro-1-phenyl-1H-pyrrole-2,5-dione 
• 853649-31-7 3,4-bis[5-(diethoxymethyl)fur-2-yl]-2,5-dihydro-1-phenyl-1H-pyrrole-2,5-dione 
• 863886-29-7 3,4-bis(2-hydroxyethylthio)-1-phenyl-1H-pyrrole-2,5-dione 
• 1451073-40-7 lithium 2,3-bis-ethylsulfanyl-3-phenylcarbamoyl-acrylate 
• 1451073-32-7 3,4-bis-ethylsulfanyl-1-phenyl-pyrrole-2,5-dione 
• 1616886-90-8 reduced somatostatin 
• 72000-67-0 3-bromo-1-phenyl-1H-pyrrole-2,5-dione 
• 5191-53-7 1,3,4-triphenyl-2,5-dihydro-1H-2,5-azoledione 

Relevant academic research and scientific papers

Maleimide derivative as well as preparation method and application thereof

The invention discloses a maleimide derivative as well as a preparation method and application thereof. The structural general formula of the maleimide derivative is shown as a formula I, wherein R1 and R2 are respectively and independently selected from

Reversible covalent linkage of functional molecules

The present invention relates to the use of a compound containing a moiety of formula (I) as a reagent for linking a compound of formula R1—H which comprises a first functional moiety of formula F1 to a second functional moiety of fo

A mild and selective protecting and reversed modification of thiols

One selective thiol-protecting study has been investigated for a wide range of thiols including general thiols and thiols containing multiple functional groups. The reactions of bromomaleimides and thiols under the mild condition afforded the protected products in excellent yields. The thiols can be recovered very quickly using dithiothreitol (DTT) under the mild condition.

Aryloxymaleimides for cysteine modification, disulfide bridging and the dual functionalization of disulfide bonds

Tuning the properties of maleimide reagents holds significant promise in expanding the toolbox of available methods for bioconjugation. Herein we describe aryloxymaleimides which represent 'next generation maleimides' of attenuated reactivity, and demonstrate their ability to enable new methods for protein modification at disulfide bonds.

Acid-cleavable thiomaleamic acid linker for homogeneous antibody-drug conjugation

In this communication we describe a novel acid-cleavable linker strategy for antibody-drug conjugation. Functional disulfide bridging of the single interchain disulfide bond of a trastuzumab Fab fragment yields a homogeneous antibody-drug conjugate bearin

LYSOSOME-CLEAVABLE LINKER

The present invention relates to a linker for forming conjugates of a protein or peptide with a therapeutically active agent and which comprise a thiomaleamic acid moiety that is susceptible to cleavage under the pH conditions prevalent in the lysosome.

A mild synthesis of N-functionalised bromomaleimides, thiomaleimides and bromopyridazinediones

Bromomaleimides are useful building blocks in synthesis and powerful reagents for the selective chemical modification of proteins. A mild new synthesis of these reagents is described, along with the convenient transferability of the approach to dithiomale

Development of antiproliferative phenylmaleimides that activate the unfolded protein response

The current paper presents the synthesis and evaluation of a series of maleimides that were designed to inhibit the Cdc25 phosphatase by alkylation of catalytically essential cysteine residues. Although in HepB3 cell culture assays the analogues did exhib

Synthesis of substituted bis(heteroaryl)maleimides

Substituted bis(fur-2-yl), bis(fur-3-yl) and bis(thien-2-yl) maleimides with potential antidiabetic properties are described. Their synthesis involves, as a key step, a Suzuki cross-coupling between various boron derivatives and the diiodomaleimides. Therefore, a wide range of substituted symmetric and non-symmetric maleimide derivatives can be prepared.

Revised Structures of N-Substituted Dibrominated Pyrrole Derivatives and Their Polymeric Products. Termaleimide Models with Low Optical Band Gaps

This paper describes an unexpected rearrangement/oxidation of N-substituted 2,5-dibromopyrroles upon treatment with HNO3. The bromides migrate from the 2,5-positions to the 3,4-positions with subsequent oxidation at the 2,5-positions to afford N-substituted 3,4-dibromomaleimides; the structure was confirmed by single-crystal X-ray analysis. The maleimides were then polymerized to the poly(N-substituted-3,4-maleimide)s with copper bronze. This constitutes a revision of structure for the monomers and polymers. The propensity for the dibromide migration was further confirmed by treatment of N-benzyl-2,5-dibromopyrrole under nonoxidative acidic conditions (p-TsOH) to afford N-benzyl-3,4-dibromopyrrole; both the starting material and product structures were confirmed by single-crystal X-ray analysis. Several termaleimides were prepared from pyrrole, maleic anhydride, and citraconic anhydride. These trimeric compounds underwent enormous shifts in their optical absorbance maxima (ca. 200 nm) when bases or nucleophilic solvents were added. Therefore, the termaleimides served as excellent models for the polymeric systems that had undergone shifts of 350-400 nm upon treatment with the same additives. Ab initio Hartree-Fock and density functional theory were utilized to assess the minimum conformation of the trimeric system. Both terminal maleimides appear canted 37° relative to the central maleimide unit. As the two end maleimide units were computationally forced into closer proximity, there was a dipolar stabilization that ensued between the two terminal maleimides with the formation of a 1,3-dioxetane. However, it is unlikely that there could be the formation of an isolable 1,3-dioxetane due to the large energy difference between the canted structure and the dioxetane. A significant decrease in the HOMO-LUMO energy of 13 kcal/mol was calculated upon formation of the 1,3-dioxetane, suggesting that nucleophiles likely move the canted structure more toward a planar form via addition to the α,β-unsaturated carbonyl units.