5455-98-1Relevant academic research and scientific papers
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.
COMPOUNDS FOR PREVENTING MIGRATION OF CANCER CELLS
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Page/Page column 62; 64, (2021/04/10)
The present invention relates to a composition for use in preventing migration of cancer cells in a subject known or suspected to suffer from cancer, the composition comprising at least one metal complex having the structure (I), formula (I), wherein M is a metal, preferably selected from the group consisting of copper, iron, manganese and zinc, X is Xa or Xb, wherein Xa is selected from the group consisting of O, S and -N(R1)-, wherein R1 is H or alkyl, and wherein Xb is a group forming a coordinate covalent bond to a second metal M', preferably a group O, S or -N(R1)-, wherein M' is preferably selected from the group consisting of copper, iron, manganese and zinc, and wherein M' and M may be the same or different and are preferably the same, Z1 and Z2, are independently of each other a, substituted or unsubstituted, -Aryl-O-, -Aryl-N- or heteroaryl group, Y is Ya or Yb, wherein Ya is selected from the group consisting of H, alkyl, -OH, -SH, halogen, and -NR3R4, wherein R3 and R4, are independently of each other selected from H and alkyl, preferably R3 and R4 are both H, and wherein Yb is a group forming a coordinate covalent bond to M or M', preferably Yb is a group O, S or -N(RYb1RYb2), wherein RYb1 and RYb1, are, independently of each other, H or alkyl, preferably H, and wherein n and m are integers, which are independently of each other, 0 or 1, Y2 is water or a halogen, and wherein Y3 is water or a halogen. The present invention further relates to a combined preparation comprising the aforesaid composition as well as to an in vitro method, for determining whether cancer cells are susceptible to immobilizing by the aforesaid compound.
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)
SUBSTITUTED 1,1'-BIPHENYL COMPOUNDS, ANALOGUES THEREOF, AND METHODS USING SAME
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Page/Page column 93, (2019/10/23)
The present invention includes substituted 3,3'-bis(phenoxymethyl)-1,1'-biphenyl compounds, analogues thereof, and compositions comprising the same, that can be used to treat or prevent hepatitis B virus (HBV) and/or hepatitis D virus (HDV) infections in a patient.
Citric acid mosapride intermediate product and application
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Paragraph 0041; 0042, (2018/09/08)
The invention belongs to the field of medical chemistry synthesis, and provides a preparation method of citric acid mosapride intermediate product IV 4-[(4-fluorophenyl)methyl]-2-morpholinemethanaminesalt and citric acid mosapride. The 2-(4-fluorobenzoamido)ethanol and 1H-Isoindole-1,3(2H)-dione,2-(2-oxiranylmethyl) are taken as raw materials, and the intermediate product IV 4-[(4-fluorophenyl)methyl]-2-morpholinemethanamine salt is obtained after acid treating is conducted; the intermediate product IV and an intermediate V 2-oxethyl-4-acetamido-5-Chlorobenzoic acid ethyl ester compounds aretaken as raw materials, dichloromethane is taken as a solvent, and EDCI and DMAP are taken as catalysts to prepare mosapride salt; the mosapride salt is reacted with citric acid aqueous solution to prepare citric acid mosapride. The intermediate product has the advantages that products are high in yield, raw materials are easy to obtain, the production cost is low, and the intermediate product issuitable for industrialized production.
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.
Method for preparing mosapride citrate intermediate
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Paragraph 0050; 0051; 0052, (2018/07/06)
The invention belongs to the technical field of medicines and particularly relates to a method for preparing a mosapride citrate intermediate IV 4-(4-fluorophenyl)-2-aminomethyl morpholine. The methodcomprises the following steps: phthalimide potassium salt and dichloro-2-propanol react to produce an intermediate II N-(2-hydroxy-3-chloropropyl) phthalimide, then the produced intermediate II and an intermediate I 2-(4-fluorphenylamine)ethyl alcohol are condensed to prepare an intermediate III N-3-[4-fluorophenyl-2-(hydroxy-ethylamine)-2-hydroxypropyl]phthalic diamide, and the intermediate IIIis subjected to cyclization and hydrolysis to obtain the intermediate IV 4-(4-fluorophenyl)-2-aminomethyl morpholine. The method is short in route, lower in production cost and suitable for industrialproduction.
A practical and enantiospecific synthesis of (-)-(R)- and (+)-(S)-piperidin-3-ols
Babu, Meruva Suresh,Raghunadh, Akula,Ramulu, Konda,Dahanukar, Vilas H.,Syam Kumar, Unniaran K.,Dubey, P. Kumar
, p. 1507 - 1515 (2015/02/19)
A highly enantiospecific, azide-free synthesis of (-)-(R)- and (+)-(S)-piperidin-3-ol in excellent yield was developed. The key step of the synthesis involves the enantiospecific ring openings of enantiomerically pure (R)- and (S)-2-(oxiran-2-ylmethyl)-1H-isoindole-1,3(2H)-diones with the diethyl malonate anion and subsequent decarboxylation.
Highly regioselective and efficient synthesis of aminoepoxides by ring closure of aminohalohydrins mediated by KF-Celite
Pace, Vittorio,Hoyos, Pilar,Sinisterra, José Vicente,Alcántara, Andrés R.,Holzer, Wolfgang
supporting information; experimental part, p. 1831 - 1834 (2011/09/16)
The regioselective synthesis of several aminoepoxides has been achieved without observing any trace of azetidinols, which are usually reported as the exclusive reaction products when aminohalohydrins are treated with bases. The use of the mild supported base KF-Celite in refluxing acetonitrile is crucial for modulating the excellent regioselectivity observed. Georg Thieme Verlag Stuttgart . New York.
