Adamantane and protoadamantanealkanamines as potential anti-Parkinson agents. 10

Abstract

The synthesis of 2-halo-1-adamantanemethanamines, 4-protoadamantanemethanamines, and 4-protoadamantaneamines is described. The anti-Parkinson activity of these amines in terms of reversal of reserpine-induced catalepsy in rats has been evaluated and compared with amantadine. 2-Bromo- and 2-chloro-1-adamantanemethanamines are shown to be twice as active as amantadine.

Mechanistic aspects of the gas-phase coupling of thioanisole and chlorobenzene to dibenzothiophene catalyzed by atomic Ho+

“…4); both processes are accessible at thermal conditions. Thus, according to the calculation, the observed ionic product Ho(C 6 (2), (3), and (5)), and the turn-over frequency is diminished due to the inefficient release of the neutral coupling product from 19 under the regeneration of Ho + ions to initiate the next catalytic cycle. As so often in heterogeneous catalysis, product release and regeneration of the active catalyst (i.e.…”

“…The overall reaction efficiency amounts to 7%, and three primary product channels were observed, i.e. reaction (4)- (6). Performing the same experiments without thermalization of the precursor Ho(C 6 H 4 S) + , the branching ratio of reaction (6) increases up to 27%, while the branching ratios of reaction (4) and (5) ligand as illustrated in Scheme 1; both routes are initiated by s bond metathesis under cleavage of the Ho-S and Ho-C bonds of the complex Ho(C 6 H 4 S) + , respectively.…”

“…[5][6][7][8] Consequently, methodological aspects related to the formation of organosulfur heterocyclic rings have attracted much attention. For the synthesis of sulfur-containing heterocycles usually metal sulfides, thioesters, or thioethers are employed as starting materials, and first-or second-row transition-metal complexes serve as catalysts.…”

Esquizofrenia: quarenta anos da hipótese dopaminérgica sob a ótica da Química Medicinal

“…Estudos de polimorfismo em receptores D 4 demonstraram que a substituição da valina-194, localizada entre os dois resíduos de serina na quinta RTM, por glicina-194, faz os neurolépticos atípicos, como clozapina (5) 25 e olanzapina (8), perderem a afinidade pelo receptor 43 . Estes mesmos estudos permitiram também observar uma redução em ca.…”

Synthesis of Spiropyrimidodiazepines and Spirodiazepinopurines by Tandem Nitroso‐ene/Diels–Alder Reactions

“…As a rule, the products possessing different substituents at C(6) and C (8) are obtained as mixtures of regioisomers, a disadvantage that is avoided by condensing 4-chloro-5-nitropyrimidines with b-amino ketones (Polonovski -Boon-type reactions) [9] [10]. Only a few examples of spirobenzodiazepines are known [4] [11] [12] and, to the best of our knowledge, no synthesis of spiropyrimido [4,5-b] [1,4]diazepines has been reported. We planned to study the nitroso-ene/Diels -Alder reaction of the tigloylamide 7 (see Scheme 2 below), the simplest amide with a substituent corresponding to CH 2 R 4 , of the methacryloyl derivative 15 (see Scheme 3 below), lacking this substituent, and of the amides 24 and 26, possessing a 6-amino, or a 6-(acylamino) instead of a benzyloxy group (see Scheme 4 below).…”