- Synthesis of benzamides through direct condensation of carboxylic acids and amines in the presence of diatomite earth@IL/ZrCl4 under ultrasonic irradiation
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A green, rapid, mild and highly efficient pathway for the preparation of benzamide derivatives is reported. The reaction was performed through direct condensation of benzoic acids and amines under ultrasonic irradiation in the presence of Lewis acidic ionic liquid immobilized on diatomite earth (diatomite earth@IL/ZrCl4). A new, highly efficient and green solid acid catalyst was easily prepared via a two-step procedure and used as an effective reusable catalyst. The prepared catalyst provides active sites for the synthesis of benzamides. The advantages of this method are the use of a superior and recoverable catalyst, low reaction times, simple procedure, high-yielding and eco-friendly process and use of ultrasonic irradiation as a green and powerful technology. Since benzamides are used widely in the pharmaceutical, paper and plastic industries, and also as an intermediate product in the synthesis of therapeutic agents, the presented new synthetic methods for this type of compounds can be of considerable importance.
- Ahmadi, Masoumeh,Moradi, Leila,Sadeghzadeh, Masoud
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p. 7873 - 7889
(2018/09/27)
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- RADIOTRACER PRECURSOR AND METHOD FOR PREPARING THE SAME
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A precursor SnBZM for a dopamine receptor radiotracer and a method for preparing the same are revealed. The precursor includes a tributyltin group (Bu3Sn) that is easy to be replaced. Thus a dopamine receptor radiotracer 123I-IBZM ca
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Paragraph 0033; 0034; 0035; 0036
(2014/03/25)
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- Dopamine D-2 receptor imaging radiopharmaceuticals: Synthesis, radiolabeling, and in vitro binding of (R)-(+)- and (S)-(-)-3-iodo-2-hydroxy-6 methoxy-N-[(1-ethyl-2-pyrrolidinyl)methyl]benzamide
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In developing central nervous system (CNS) dopamine D-2 receptor imaging agents, enantiomers, R-(+) and S-(-) isomers, of 3-[125I]iodo-2-hydroxy-6-methoxy-N-[(1-ethyl-2-pyrrolidinyl)methyl]d benzamide, [125I]IBZM, were synthesized, and their in vitro binding characteristics were evaluated in rat striatum tissue preparation. The (S)-(-)-[125I]IBZM showed high specific dopamine D-2 receptor binding (K(d) = 0.43 nM, B(max) = 0.48 pmol/mg of protein). Competition data of various ligands for IBZM binding displayed the following rank order of potency: spiperone > (S)-(-)-IBZM > (+)-butaclamol >> (R)-(+)-IBZM > (S)-(-)-BZM > dopamine > ketanserin > SCH23390 >> propranolol. The results indicate that [125I]IBZM binds specifically to the dopamine D-2 receptor with stereospecificity. The [123I][IBZM is potentially useful as an imaging agent for the investigation of dopamine D-2 receptors in humans.
- Kung,Kasliwal,Pan,Kung,Mach,Guo
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p. 1039 - 1043
(2007/10/02)
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- Potential neuroleptic agents. 3. Chemistry and antidopaminergic properties of substituted 6-methoxysalicylamides
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A series of substituted 6-methoxysalicylamides were synthesized from their corresponding 2,6-dimethoxybenzamides by demethylation of one methoxy group with boron tribromide. Substituted 6-methoxysalicylamides having a lipophilic aromatic substituent in the 3-position para with respect to the methoxy group, e.g. a bromo or an iodo atom or an ethyl or a propyl group, and having an (S)-N-(1-alkyl-2-pyrrolidinyl)methyl moiety as the side chain were found to be potent blockers of [3H]spiperone binding in vitro and potent inhibitors of the apomorphine syndrome in the rat. Similar to remoxipride but in contrast to haloperidol, some of the substituted salicylamides show a 10-20 fold separation between the dose that inhibits hyperactivity and that which inhibits stereotypy. It was concluded that, besides the requirement of a lipophilic substitutent in the position para to the methoxy group for antidopamine activity in vivo, the formation of a coplanar six-membered pseudoring involving the amide moiety and the methoxy group is a structural requirement for activity in vitro.
- de Paulis,Kumar,Johansson,Raemsby,Florvall,Hall,Angeby-Moeller,Ogren
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p. 1263 - 1269
(2007/10/02)
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