Pharmaceutically active compounds

The imidazole ring is a privileged structure in medicinal chemistry since it is found in the core structure of a wide range of pharmaceutically active compounds efficient methods for the preparation of substituted imidazole libraries are therefore of great interest. Recently, a rapid synthetic route to imidazole-4-carboxylic acids using Wang resin was reported by Henkel (Fig. 17) [64]. An excess aliphatic or aromatic amine was added to the commercially available Wang-resin-bound 3-Ar,M-(dimethylamino)isocyano-acrylate, and the mixture was heated in a sealed vial with microwave irradi-... 

Santos JL, Aparicio I, Alonso E (2007) Occurrence and risk assessment of pharmaceutically active compounds in wastewater treatment plants. A case study Seville city (Spain). Environ Int 33 596-601... 

Sedlak DL, Pinkston K, Huang CH (2005) Occurrence survey of pharmaceutically active compounds. Awwa Reserch Foundation, Denver, CO... 

The focus of this paper is on the preparation of biaryl moieties which are commonly present in a wide variety of pharmaceutically active compounds. Two different and practical approaches to synthesize the biaryl substructure will... 

The occurrence of the indole subunit is well established within the class of natural products and pharmaceutically active compounds. Recently, the Reissig group developed an impressive procedure for the assembly of highly functionalized in-dolizidine derivatives, highlighting again the versatility of domino reactions [8]. The approach is based on a samarium(II) iodide-mediated radical cydization terminated by a subsequent alkylation which can be carried out in an intermolecular - as well as in an intramolecular - fashion. Reaction of ketone 3-11 with samarium(ll) iodide induced a 6-exo-trig cydization, furnishing a samarium enolate intermediate... 

Enzymes are useful catalysts for a broad diversity of chemical reactions that enable the synthesis of natural and unnatural highly pure pharmaceutically active compounds. However, proteins themselves can also be the pharmaceutical ingredients. 

Santos JL, Aparicio I, Callejon M, Alonso E (2009) Occurrence of pharmaceutically active compounds during 1-year period in wastewaters from four wastewater treatment plants in Seville (Spain). J Hazard Mater 164 1509-1516... 

Scheme 24.12 Several pharmaceutically active compounds to have been synthesized via Rh-phospholane-mediated asymmetric hydrogenation.

Table 1. The diverse range of pharmaceutically active compounds that have been incorporated into nanoparticles or nanocapsules.

Modem HPLC finds its abundant applications not only confined to isolation of natural pharmaceutically active compounds, control of microbiological processes but also assay of pure drugs and their dosage forms. A few typical examples will be discussed below ... 

Diarylethenes, 1,1-diarylallylalcohols and aryl vinyl ethers were succesfully hydroformylated in water/toluene or water/cyclohexane biphasic mixtures with a catalyst prepared in situ from[ RhCl(COD) 2] and TPPTS (Scheme 4.15). Yields of the desired linear aldehyde product were around 80%. This method was applied for the synthesis of the neuroleptics Fluspirilen and Penfluridol (Scheme 4.16) and for other pharmaceutically active compounds containing the 4,4-bis(p-fluorophenyl)butyl group [153]. 

Kimura K, Amy G, Drewes JE, Heberer T, Kim T-U, Watanabe Y (2003) Rejection of organic micropollutants (disinfection by-products, endocrine dismpting compounds, and pharmaceutically active compounds) by NF/RO membranes. J Membr Sci 227 113-121... 

Kimura K, Toshima S, Amy G, Watanabe Y (2004) Rejection of neutral endocrine disrupting compounds (EDCs) and pharmaceutical active compounds (PhACs) by RO membranes. J Membr Sci 245 71... 

Hawkshead JJ (2008) Hospital wastewater containing pharmaceuticals active compounds and drag-resistant organisms a source of environmental toxicity and increased antibiotic resistance. J Residual Sci Tech 5 51-60... 

Bendz D (2005) Occurrence and fate of pharmaceutically active compounds in the environment, a case-study Hoje River in Sweden. J Hazard Mater 122 195-204... 

Alkaloids are pharmaceutically active compounds contained in plants. Some of them exhibit also important toxic properties and may be encountered in forensic toxicology as a cause of accidental, suicidal, or homicidal poisonings. 

More than 100 pharmaceutically active compounds of various prescription classes have been detected in water, livestock-derived manure, sewage, sediments, potable water, biosohds, and soil. The compounds detected belong to a wide range of classes of PPCPs, including antibiotics, antiphlogistics, antiepileptics, beta blockers, hpid regulators, vasodilators, and sympathomimetics. Most of the evidence for the presence of these compounds in the environment has been accumulated in aquatic systems. Occurrence in different matrices is also discussed. 

Molecular Size of the Compounds The size and molecular length of the PPCP compound can also influence the efficacy of the membrane. Molecular length is, in this instance, defined as the maximum length of the molecule, whereas molecular width refers to its cross-sectional diameter. Kimura et al. (2003) tested 11 neutral pharmaceutically active compounds that greatly vary in molecular weight, octanol-water partition coefficients (Xqw), and dipole moments for regeneration by two distinctly different RO membranes. AU of the assays were conducted at 20°C (pH 7 + 0.1) and filtration was done over a 24-h period. A key assumption from that experiment was that by the end of that duration, the membrane was saturated. The percent regeneration K) of the compound by the membrane was calculated from... 

Brown K.D. (2004). Pharmaceutically active compounds in residential and hospital effluent, municipal wastewater, and the Rio Grande in Albuquerque, New Mexico. Water Resource Program, University of New Mexico, Albuquerque, NM. Publication No. WRP-9. 

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