83502-69-6

Upstream product

• 10297-05-9 1-chloro 4-iodobutane 
• 91-56-5 indole-2,3-dione 
• 6940-78-9 4-chlorobutyl bromide 
• 110-56-5 1,4-dichlorobutane 

Relevant academic research and scientific papers

Synthesis of N-(2-chloroethyl)isatins and their β-ethyleneacetals and β-thiosemicarbazones

The nitrogen atoms of isatin, its 5-bromo derivative, and their β-ethyleneacetals are alkylated by 1,2-dichloroethane in K2CO3-DMF and LiH(NaH)-DMF. 1999 KluwerAcademic/Plenum Publishers.

Chiral Lewis Acid Catalyzed Reactions of α-Diazoester Derivatives: Construction of Dimeric Polycyclic Compounds

An unexpected homologation/dyotropic rearrangement/interconversion/[3+2] cycloaddition cascade reaction of α-diazoester-terminated N-propyl-substituted isatin derivatives was achieved in the presence of a chiral N,N′-dioxide/ScIII catalyst. This catalytic manifold allows rapid construction of several classes of dimeric polycyclic compounds with good yields and high levels of diastereo- and enantioselectivity (up to 99 % ee). Furthermore, macrocyclic dimers can be obtained by an intermolecular homologation process.

Design, synthesis, in silico studies and in vitro evaluation of isatin-pyridine oximes hybrids as novel acetylcholinesterase reactivators

Organophosphorus poisoning caused by some pesticides and nerve agents is a life-threating condition that must be swiftly addressed to avoid casualties. Despite the availability of medical countermeasures, the clinically available compounds lack a broad spectrum, are not effective towards all organophosphorus toxins, and have poor pharmacokinetics properties to allow them crossing the blood-brain barrier, hampering cholinesterase reactivation at the central nervous system. In this work, we designed and synthesised novel isatin derivatives, linked to a pyridinium 4-oxime moiety by an alkyl chain with improved calculated properties, and tested their reactivation potency against paraoxon- and NEMP-inhibited acetylcholinesterase in comparison to the standard antidote pralidoxime. Our results showed that these compounds displayed comparable in vitro reactivation also pointed by the in silico studies, suggesting that they are promising compounds to tackle organophosphorus poisoning.

Novel metal chelators thiosemicarbazones with activity at the σ2 receptors and P-glycoprotein: An innovative strategy for resistant tumor treatment

To combat the emergence of drug-resistance in tumors novel strategies are urgently needed. With this in mind we designed a novel class of thiosemicarbazones able to target simultaneously σ2 receptors and P-glycoprotein efflux pump while chelating metals such as iron. The combined effect of these targets would lead to the activation of multiple pathways to which resistant tumors are sensitive. Indeed, most of the novel thiosemicarbazones displayed antiproliferative activity in both parent (MCF7 breast adenocarcinoma and A549 lung carcinoma) and corresponding doxorubicin-resistant cells (MCF7dx and A549dx). A few compounds emerged for their potent antiproliferative activity or for their more potent effect in doxorubicin-resistant cells than in the parent ones, while other compounds emerged for their remarkable P-gp modulatory activity. These results pave the way for further studies on these targets in the oncology field, while the availability of promising molecules for resistant tumors treatment that warrant deeper investigations was increased.

Hexahydro-trans- and tetrahydropyridoindole neuroleptic agents

Derivatives of 2,3,4,5-tetrahydro-1H-pyrido[4,3-b]-indole and of (+)enantiomeric, mixtures of (+) and (-)enantiomeric or (±)racemic 2,3,4,4a,5,9b-hexahydro-4a,9b-trans-1H-pyrido[4,3-b]indole, substituted at the 5-position with an aryl group and at the 2-p