烃化剂的显色剂——4-(对硝基苄基)吡啶(NBP)的合成

Klatt曾报导,以4-(对硝基苄基)吡啶用比色法则定血液中烃化剂的含量.关于此种显色剂的制备,文献中有关它的前体——4-苄基吡啶的合成方法报告较多.但反应产物都是2-与4-苄基吡啶混合物,必须经细致分离,而且收率亦低.Jerchel等报导4-氯代甲基吡咤盐酸盐与苯翘过Friedel-Crafts反应得到4-苄基吡啶,收率较高(75％).由于原料难得,因此作者设计了以异烟酸为原料的下列合成路线,所得4-苄基吡啶的总收率达51％.不仅不可能有化合物Ⅲ的异构体,而且原料易得,实验条件也较易控制.     

Correlation of mutagenicity and 4-(p-nitrobenzyl)-pyridine alkylation by epoxides

The reactivity of simple epoxides with 4-(p-nitrobenzyl)-pyridine was compared with their mutagenicity in Salmonella typhimurium TA 100 and Escherichia coli WP 2 uvrA. The order of reactivity correlated well with mutagenicity, trichloropropylene oxide being most potent followed by epichlorohydrin, styrene oxide, glycidol and propylene oxide. The results suggest that 4-(p-nitrobenzyl)-pyridine alkylation is a simple and reliable primary assay in the evaluation of mutagenic properties.     

Alkylation of guanosine and 4-(p-nitrobenzyl)-pyridine by styrene oxide analogues in vitro

In vitro alkylation activity of styrene oxide (SO) and three of its analogues, 4-vinyltoluene oxide (VTO), 3,5-dimethylstyrene oxide (DMSO), and 4-nitrostyrene oxide (NSO) was assayed using 4-(p-nitrobenzyl) pyridine (NBP) and guanosine as nucleophiles. Hydrolysis rates were also determined. The half-lives of VTO, DMSO, SO, and NSO were 8, 11, 40, and 60 h, respectively in aqueous solution. The rate of NBP alkylation correlated with the rate of hydrolysis. By contrast, the rates of guanosine alkylation were quite different: SO > VTO > DMSO. NSO did not react with guanosine. Fluorescence and ultraviolet spectroscopic data on the guanosine adducts indicated that SO, VTO, and DMSO formed main alkyl products at N-7.     

Chemistry and pharmacology of compounds related to 4-(4-hydroxy-4-phenyl-piperidino)-butyrophenone

Summary Haloperidol (R 1625) is 50 to 100 times more active than chlorpromazine as an inhibitor of exploratory motor behaviour in rats. Emotional defaecation in rats is inhibited by both drugs at similar dose levels.Thanks are due to Mr. Remi Frederickx for his technical assistance.