5455-98-1Relevant articles and documents
Synthesis of α-phthalimido-α′-dithiocarbamato propan-2-ols via a one-pot, three-component epoxide ring-opening in water
Halimehjani, Azim Ziyaei,Hooshmand, Seyyed Emad,Shamiri, Elham Vali
, p. 5454 - 5457 (2014)
Regioselective ring-opening of the N-(2,3-epoxypropyl)phthalimide with in situ prepared dithiocarbamic acid in water is reported for the synthesis of a new family of α-phthalimido-α′-dithiocarbamato propan-2-ols. The present method is simple, EtOAc is used for work-ups and affords excellent yield of products.
Poly(glycidyl amine) and copolymers with glycidol and glycidyl amine repeating units: Synthesis and characterization
Meyer, Joerg,Keul, Helmut,Moeller, Martin
, p. 4082 - 4091 (2011)
The synthesis and characterization of poly(glycidol-co-glycidyl amine), poly(glycidol)-block-poly(glycidyl amine), and poly(glycidol) end-capped with a glycidyl amine unit is reported. Copolymerization of ethoxyethyl glycidyl ether with epichlorohydrin using tetraoctylammonium bromide/triisobutylaluminium as catalyst leads to statistical or block copolymers. Sequential addition of the monomers to the initiator leads to block copolymers while simultaneous copolymerization of the monomers results in statistical copolymers. The resulting polyethers with protected hydroxymethyl and chloromethyl side groups were converted in three steps to poly(epoxide)s with hydroxymethyl and aminomethyl side chains. These polymers have a high potential for the preparation of multifunctional polymers since amine and alcohol groups can be addressed selectively by electrophiles. An intermediate in the synthesis of these functional poly(epoxide)s are polyethers with hydroxymethyl and azidomethyl side chains. The azide group of these copolymers was further functionalized via a click reaction with propargyl alcohol proving the reactivity of the polymer bound azide group. Furthermore, preparation of poly(glycidol)s bearing a glycidyl amine end group is reported.
A 5 - aminolevulinic acid hydrochloride of new synthetic method (by machine translation)
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Paragraph 0009-0010, (2019/05/16)
The invention belongs to the field of organic synthesis, in particular relates to a 5 - aminolevulinic acid hydrochloride new synthesis method. The synthesis method the new synthesis method ech as the starting material, by Gabriel reaction, ring-opening, oxidation, substituted, hydrolysis reaction steps such as to obtain the target product 5 - aminolevulinic acid hydrochloride. The invention uses a 5 - aminolevulinic acid hydrochloride new synthesis method, can significantly speed up the reaction rate and to improve the yield, while at the same time little side reaction, the operation is simple, after treatment is convenient, and is suitable for industrial production. (by machine translation)
Design, synthesis, and biological evaluation of 2-(benzylamino-2-hydroxyalkyl)isoindoline-1,3-diones derivatives as potential disease-modifying multifunctional anti-Alzheimer agents
Panek, Dawid,Wi?ckowska, Anna,Pasieka, Anna,Godyń, Justyna,Jończyk, Jakub,Bajda, Marek,Knez, Damijan,Gobec, Stanislav,Malawska, Barbara
, (2018/02/14)
The complex nature of Alzheimer's disease calls for multidirectional treatment. Consequently, the search for multi-target-directed ligands may lead to potential drug candidates. The aim of the present study is to seek multifunctional compounds with expected activity against disease-modifying and symptomatic targets. A series of 15 drug-like various substituted derivatives of 2-(benzylamino-2-hydroxyalkyl)isoindoline-1,3-diones was designed by modification of cholinesterase inhibitors toward β-secretase inhibition. All target compounds have been synthesized and tested against eel acetylcholinesterase (eeAChE), equine serum butyrylcholinesterase (eqBuChE), human β-secretase (hBACE-1), and β-amyloid (Aβ-aggregation). The most promising compound, 12 (2-(5-(benzylamino)-4-hydroxypentyl)isoindoline-1,3-dione), displayed inhibitory potency against eeAChE (IC50 = 3.33 μM), hBACE-1 (43.7% at 50 μM), and Aβ-aggregation (24.9% at 10 μM). Molecular modeling studies have revealed possible interaction of compound 12 with the active sites of both enzymes-acetylcholinesterase and β-secretase. In conclusion: modifications of acetylcholinesterase inhibitors led to the discovery of a multipotent anti-Alzheimer's agent, with moderate and balanced potency, capable of inhibiting acetylcholinesterase, a symptomatic target, and disease-modifying targets: β-secretase and Aβ-aggregation.
