Dennis J. Hlasta

Tandem organometallic addition reactions to N-methoxy-ureas and urethanes in the preparation of unsymmetrical and symmetrical ketones

Abstract The use of the novel reagents 1a–c for the synthesis of ketones in a one pot reaction is described. An interesting leaving group effect was discovered in the fragmentation of the proposed complexes 2 to the intermediate N-methoxyamides 3 .

The synthesis of substituted saccharins through the o-lithiative sulfonamidation of N,N-diethylbenzamides

Abstract The readily available N,N-diethylbenzamides 2 are converted in two reaction steps to a variety of substituted saccharins 4 in good overall yields.

Regiospecific acylation reactions of imidazo[1,5-a]pyridine

Abstract Imidazo [1,5-alpyridine ( 1 ) displays dual reactivity through two condition-dependent reaction pathways. Regiospecific acylation occurs with benzoyl chloride at the 1-position under Friedl-Crafts conditions to afford 3 or at the 3-position via a postulated, stabilized ylid 5 under thermal or triethylamine-mediated acylation conditions to give 2 .

Dianion metallation reactions of N,N-dimethylvanillylamine and N,N-dimethylisovanillylamine

The utility of dianion chemistry in the synthesis of polyfunctional aromatics is demonstrated by the direct lithiation of the vanillylamine 1 and by the metal-halogen exchange reaction of the bromo isovanillylamines 9 and 10.

Chapter 3 Antidepressant Agents

Publisher Summary The major concerns in current anti-depression therapy are delayed onset of activity, less than ideal efficacy, the importance of proper patient selection, and biochemical predictors of treatment response and side effects. There are various obstacles. Urinary 3-methoxy-4-hydroxyphenylglycol (MHPG) levels appear not to predict the treatment response. Platelet serotonin (5-HT) uptake does not show a circadian rhythm in delusional and nondelusional depressed patients unlike healthy subjects. Placebo responders are likely to be nonendogenous depressives and have a shorter length of illness with less severe symptomatology. The search has continued to identify new “second generation” monoamine uptake inhibitors and to identify selective inhibitors of monoamine oxidase A or B. The α 2 -adrenergic antagonists offer a new therapy for the treatment of depression, although the efficacy of these agents is yet to be studied conclusively in human. Data pertaining to the effects of depressive illness and treatment with anti-depressants on %-adrenergic receptors have been studied. Platelet α 2 -adrenoceptors appeared to be elevated in drug-free depressed patients and anti-depressant treatment returned these values to normal. A more rapid onset of anti-depressant effect and fewer adverse drug effects than existing therapeutic agents remain as the important hurdles for the newer agents undergoing clinical evaluation.