96947-76-1Relevant articles and documents
Synthesis of benzamides through direct condensation of carboxylic acids and amines in the presence of diatomite earth@IL/ZrCl4 under ultrasonic irradiation
Ahmadi, Masoumeh,Moradi, Leila,Sadeghzadeh, Masoud
, p. 7873 - 7889 (2018/09/27)
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.
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
Kung,Kasliwal,Pan,Kung,Mach,Guo
, p. 1039 - 1043 (2007/10/02)
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.
