Racemic 2-n-butylbutanedioic acid 4-t-butyl esters were synthesized from methyl hexanoate and t-butyl α-iodoacetate via alkylation and subsequently selective hydrolyzation. The （R）-and （S）-2-n-butylbutanedioic ac...Racemic 2-n-butylbutanedioic acid 4-t-butyl esters were synthesized from methyl hexanoate and t-butyl α-iodoacetate via alkylation and subsequently selective hydrolyzation. The （R）-and （S）-2-n-butylbutanedioic acid 4-t-butyl esters were obtained by the resolution of the above-mentioned racemic compounds with（S）-（ - ） or（R）-（ ＋ ）-α- methylbenzylamine, respectively. The e.e. values of the two optical active products were determined to be above 99% by HPLC after the formation of two pairs of diastereoisomers with（R）-（ ＋ ）-α-methylbenzylamine and（S）- phenylalanine methyl ester.展开更多
2-Acetyl-hexanoic acid ethyl ester is one of important derivatives.It has been used widely useful materials as anesthetics,spice,medicine and so on.The reaction liquid of acetyl-acetic acid ethyl ester with n-butane b...2-Acetyl-hexanoic acid ethyl ester is one of important derivatives.It has been used widely useful materials as anesthetics,spice,medicine and so on.The reaction liquid of acetyl-acetic acid ethyl ester with n-butane bromide was analyzed by gas chromatograph-mass spectrometry.The results show that there are four kinds of compounds in the reaction liquid.The main yield is 2-acetyl-hexanoic acid ethyl ester,while by-products are 2-acetyl-2-butyl-hexanoic acid ethyl ester and 3-butoxy-2-butenoic acid ethyl ester.展开更多
Despite the many years of extensive research using rodent models to study Alzheimer＇s disease （AD）, no cure or disease halting drug exists. An increasing number of people are suffering from the disease and a therap...Despite the many years of extensive research using rodent models to study Alzheimer＇s disease （AD）, no cure or disease halting drug exists. An increasing number of people are suffering from the disease and a therapeutic intervention is needed. Therefore, it is necessary to have complementary models to aid in the drug discovery. The zebrafish animal model is emerging as a valuable model for the investigation of AD and neurodegenerative drug discovery. The main genes involved in human AD have homologous counter- parts in zebrafish and have conserved function. The basic brain structure of the zebrafish is also conserved when compared to the mammalian brain. Recently an AD model was established by administering okadaic acid to zebrafish. It was used to test the efficacy of a novel drug, lanthionine ketimine-5-ethyl ester, and to elucidate its mechanism of action. This demonstrated the ability of the okadaic acid-induced AD zebrafish model to be implemented in the drug discovery process for therapeutics against AD.展开更多
基金Supported by the National Basic Research Priority Program(No. 2003CCA027).
文摘Racemic 2-n-butylbutanedioic acid 4-t-butyl esters were synthesized from methyl hexanoate and t-butyl α-iodoacetate via alkylation and subsequently selective hydrolyzation. The （R）-and （S）-2-n-butylbutanedioic acid 4-t-butyl esters were obtained by the resolution of the above-mentioned racemic compounds with（S）-（ - ） or（R）-（ ＋ ）-α- methylbenzylamine, respectively. The e.e. values of the two optical active products were determined to be above 99% by HPLC after the formation of two pairs of diastereoisomers with（R）-（ ＋ ）-α-methylbenzylamine and（S）- phenylalanine methyl ester.
文摘2-Acetyl-hexanoic acid ethyl ester is one of important derivatives.It has been used widely useful materials as anesthetics,spice,medicine and so on.The reaction liquid of acetyl-acetic acid ethyl ester with n-butane bromide was analyzed by gas chromatograph-mass spectrometry.The results show that there are four kinds of compounds in the reaction liquid.The main yield is 2-acetyl-hexanoic acid ethyl ester,while by-products are 2-acetyl-2-butyl-hexanoic acid ethyl ester and 3-butoxy-2-butenoic acid ethyl ester.
文摘Despite the many years of extensive research using rodent models to study Alzheimer＇s disease （AD）, no cure or disease halting drug exists. An increasing number of people are suffering from the disease and a therapeutic intervention is needed. Therefore, it is necessary to have complementary models to aid in the drug discovery. The zebrafish animal model is emerging as a valuable model for the investigation of AD and neurodegenerative drug discovery. The main genes involved in human AD have homologous counter- parts in zebrafish and have conserved function. The basic brain structure of the zebrafish is also conserved when compared to the mammalian brain. Recently an AD model was established by administering okadaic acid to zebrafish. It was used to test the efficacy of a novel drug, lanthionine ketimine-5-ethyl ester, and to elucidate its mechanism of action. This demonstrated the ability of the okadaic acid-induced AD zebrafish model to be implemented in the drug discovery process for therapeutics against AD.
