Pharmacological activity synthesis

The appearance of the 2-(indol-3yl)ethylamine (tryptamine) unit in both tryptophan-derived natural products and in synthetic materials having potential pharmacological activity has generated a great deal of interest in the synthesis of such compounds. Several procedures which involve either direct 3-alkylation or tandem 3-functionalization/modification have been developed. Similarly, methodology applicable to preparation of tryptophan analogues has been widely explored. 

Various borate esters are chemostetilants for house flies (51). Tributyl borate, available from Eagle-Picher, Miami, Oklahoma, which is isotopically enriched in boron-10, is being used as a chemical precursor in the synthesis of pharmacologically active boron compounds suitable for boron neutron capture therapy. 

Dibenzo[b,/]thiepin, 10,11 -dihydroapplications, 7, 591 pharmacological activity, 7, 591 Dibenzothiepins synthesis, 7, 588 Dibenzo[6,/ thiepins applications, 7, 592 synthesis. 7. 587... 

Imidazolidin-2-one, l-(5-nitro-2-thiazolyl)-pharmacological activity, 6, 328 Imidazolidin-4-one, l-aryl-3-phenyl-2-thioxo- C NM S, 355 Imidazolidinones C NMR, 5, 355 Imidazolidin-2-ones nucleophilic displacement, 5, 428 polymers, 1, 279-280 reactivity, 5, 376 synthesis, 5, 466, 471 Imidazolidin-4-ones synthesis, 5, 468 Imidazoline, 2-alkyl-synthesis, 5, 463 Imidazoline, 2-amino-applications, 5, 498 Imidazoline, 2-aryl-synthesis, 5, 463 Imidazoline, 2-methyl-synthesis, 5, 487 Imidazoline, 2-nitroamino-synthesis, 5, 471 2-Imidazoline, 2-arylamino-tautomerism, 5, 368 2-Imidazoline, 1-benzyl-methylation, 5, 425 2-Imidazoline, 1,2-diaryl-synthesis, 5, 463... 

Quaternary salts of the substances represented by tliese formulae have been prepared by Kogl, Veldstra and van der Laan as well as of the next lower homologues, the substituted butyraldehydes, and the methyl ethers of both series. Their pharmacological activities were negligible in comparison with that of muscarine, but as six stereoisomeric forms may be produced in each synthesis, the inactivity may be due to stereoisomerism, just as in the case of threonine (a-amino-)3-hydroxy-butyric acid) where West and Carter found that only the d —) form is... 

The Mannich reactions plays an important role in pharmaceutical chemistry. Many /3-aminoalcohols show pharmacological activity. The Mannich reaction can take place under physiological conditions (with respect to pH, temperature, aqueous solution), and therefore can be used in a biomimetic synthesis e.g. in the synthesis of alkaloids. 

Vinylindoles have been studied extensively and used in the synthesis of carbazoles, alkaloids and other classes of pharmacologically active compounds. MMX force field calculations have shown that coplanar s-cis and. s-trans conformations of 3-vinylindole (84, Figure 2.11) are the most stable conformers they exhibit only slight differences in their thermodynamic stabilities [86]. 

The technical aspect of 2-bromo-a-ergocryptine synthesis, including the characterisation and significance of the impurities obtained in the production process, were reviewed. In the continuation new ergolene and ergoline compounds were synthesized and tested for the pharmacological activity. 

The lH-l,2,4-triazole compounds possess important pharmacological activities such as antifimgal and antiviral activities [18-20]. In the present study, the reactive intermediates 45a-c, prepared in situ from the dichlorides 44a-c, were reacted via the cycloaddition reaction with ethyl cyanoacetate 40 to give, after spontaneous rearrangement, the triazole hydrazides 41a-c. These compoimds were used as starting materials for the synthesis of the... 

Due to its marked atom economy, the intramolecular hydroamination of alkenes represents an attractive process for the catalytic synthesis of nitrogen-containing organic compounds. Moreover, the nitrogen heterocycles obtained by hydroamination/cyclisation processes are frequently found in numerous pharmacologically active products. The pioneering work in this area was reported by Marks et al. who have used lanthanocenes to perform hydroamination/cyclisation reactions in 1992. These reactions can be performed in an intermolecular fashion and transition metals are by far the more efficient catalysts for promotion of these transformations via activation of the... 

Phenyl cycloalkylamine derivatives. II. Synthesis and pharmacological activity. J. Hed Chem 12 473-477, 1969. 

In the discovery phase, a reaction route is developed to allow synthesis of a maximum number of analogues for pharmacological testing. Since the focus is on synthetic flexibility, issues of scale are not central. Once a lead compound exhibits a useful pharmacological activity and is identified as a candidate for further development, larger scale synthesis is required to evaluate stability, bioavailability, toxicity, physicochemical properties, and other compound properties. The Chemical Development Department is usually involved in the preparation of supplies for these activities. 

A one-pot synthesis of pyrano[3,2-c]quinolin-2,5(<5/7)-dione 107 was reported through the condensation reaction of chlorocarbonyl ketenes 108 with 4-hydroxyquinolin-2(l//)-ones 109. This simple procedure was shown to be a convenient synthesis of pharmacologically active compounds in high yields <06S435>. 

Utilizing the same aryl fluoride linker on conventional MeOPEG polymer, these authors also presented a microwave-accelerated liquid-phase synthesis of benzimidazoles (Scheme 7.70) [79]. This bicydic pharmacophore is an important and valuable structural element in medicinal chemistry, showing a broad spectrum of pharmacological activities, such as antihistaminic, antiparasitic, and antiviral effects. 

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