Acquired neurological injuries initiate a pathological cascade of secondary injury processes,including inflammation,which continue for days to weeks following injury.Injury-induced neuroinflammation acts as a host def...Acquired neurological injuries initiate a pathological cascade of secondary injury processes,including inflammation,which continue for days to weeks following injury.Injury-induced neuroinflammation acts as a host defense mechanism contributing to the neutralization of the insult(removing offending factors)and restoring structure and function of the brain(establish homeostasis).The timing of these protective functions of the immune response is vital,since chronic inflammation展开更多
Synthesis and photochemistry of acridin-9-ylmethoxycarbonyl (Amoc) as a new photochemically removable protecting group for alcohols were described. Three carbonates of alcohols 1-3 were synthesized through condensat...Synthesis and photochemistry of acridin-9-ylmethoxycarbonyl (Amoc) as a new photochemically removable protecting group for alcohols were described. Three carbonates of alcohols 1-3 were synthesized through condensation of 9-hydroxymethylacridine and chloroformates of alcohols, including benzyl alcohol, phenethyl alcohol and one galactose derivative. The photolysis of protected alcohols can efficiently release the corresponding alcohol in the efficiencies (Qulε) of 100-200 (quantum yield Qul=0.011-0.023, and molar absorptivity ε= 9.1 × 10^3-9.8 × 10^3 mol^-1·L·cm^-1) under 360 nm light.展开更多
Benzyl protecting protocol was first employed in two routes for the concise synthesis of dopexamine dihydrochloride.This protecting group could be cleanly removed under mild condition and no unacceptable ion was broug...Benzyl protecting protocol was first employed in two routes for the concise synthesis of dopexamine dihydrochloride.This protecting group could be cleanly removed under mild condition and no unacceptable ion was brought to the final product.The total yield of route I was 43.8% from phenylacetic acid,while it was 54.1% of route II from 2-(3,4-bis(benzyloxy)phenyl)acetic acid.The titration purity of the final product was more than 99.5%,while any single or total impurities met the known standard of the drug by HPLC analysis.The measured residual palladium met an acceptable limit(〈1 ppm) as an API for injection.展开更多
文摘Acquired neurological injuries initiate a pathological cascade of secondary injury processes,including inflammation,which continue for days to weeks following injury.Injury-induced neuroinflammation acts as a host defense mechanism contributing to the neutralization of the insult(removing offending factors)and restoring structure and function of the brain(establish homeostasis).The timing of these protective functions of the immune response is vital,since chronic inflammation
基金Project supported by the National Natural Science Foundation of China (No. 30470444).
文摘Synthesis and photochemistry of acridin-9-ylmethoxycarbonyl (Amoc) as a new photochemically removable protecting group for alcohols were described. Three carbonates of alcohols 1-3 were synthesized through condensation of 9-hydroxymethylacridine and chloroformates of alcohols, including benzyl alcohol, phenethyl alcohol and one galactose derivative. The photolysis of protected alcohols can efficiently release the corresponding alcohol in the efficiencies (Qulε) of 100-200 (quantum yield Qul=0.011-0.023, and molar absorptivity ε= 9.1 × 10^3-9.8 × 10^3 mol^-1·L·cm^-1) under 360 nm light.
基金supported by Program for Innovative Research Team of the Ministry of Education and Program for Liaoning Innovative Research Team in UniversityShenyang Shuangding Pharmaceutical Co.,LTD.,Shenyang,China
文摘Benzyl protecting protocol was first employed in two routes for the concise synthesis of dopexamine dihydrochloride.This protecting group could be cleanly removed under mild condition and no unacceptable ion was brought to the final product.The total yield of route I was 43.8% from phenylacetic acid,while it was 54.1% of route II from 2-(3,4-bis(benzyloxy)phenyl)acetic acid.The titration purity of the final product was more than 99.5%,while any single or total impurities met the known standard of the drug by HPLC analysis.The measured residual palladium met an acceptable limit(〈1 ppm) as an API for injection.