The two diarylheptanoids (E)-1-(4-hydroxy-3-methoxyphenyl)-7-(4-hydroxyphenyl) hept-4-en-3-one 1 (Gingerenone C) and (±)-5-hydroxy-1-(4-hydroxy-3-methoxyphenyl)-7-(4- hydroxyphenyl)-3-heptanone 2 were synthesized...The two diarylheptanoids (E)-1-(4-hydroxy-3-methoxyphenyl)-7-(4-hydroxyphenyl) hept-4-en-3-one 1 (Gingerenone C) and (±)-5-hydroxy-1-(4-hydroxy-3-methoxyphenyl)-7-(4- hydroxyphenyl)-3-heptanone 2 were synthesized from vanillin 3 and 4-hydroxybenzaldehyde 9.展开更多
The title compound, （E）-1-（7-methoxy-2,2-dimethyl-2,3-dihydrobenzofuran-5-yl）- 3-（2-methoxyphenyl）-2-（1H-1,2,4-triazol-1-yl）propenol （3a）, was synthesized by the Aldol con- densation reaction of 1-（7-methox...The title compound, （E）-1-（7-methoxy-2,2-dimethyl-2,3-dihydrobenzofuran-5-yl）- 3-（2-methoxyphenyl）-2-（1H-1,2,4-triazol-1-yl）propenol （3a）, was synthesized by the Aldol con- densation reaction of 1-（7-methoxy-2,2-dimethyl-2,3-dihydrobenzofuran-5-yl）-2-（1,2,4-triazol- 1-yl）ethanone with 2-methoxybenzaldehyde and then reduced with NaBH4, and its crystal structure was determined by single-crystal X-ray diffraction： monoclinic system, space group P21 with a = 6.2002（3）, b = 12.8452（7）, c = 13.2257（7） ？, Z = 2, V = 1031.23（9） ？3, Mr = 407.46, Dc = 1.312 Mg/m3, S = 1.054, μ = 0.091 mm-1, F（000） = 432, the final R = 0.0353 and wR = 0.0769 for 3161 observed reflections （I 〉 2σ（I））. X-ray analysis displays that the title compound adopts an E configuration for the C（7）=C（8） double bond and S configuration for the chirality center with the specific rotation of –63.75°. Furthermore, the stability of the crystal was maintained through the intermolecular hydrogen bond O（1）–H？？？N（3）. The antitumor assay exhibits that the title compound 3a （E configuration） has a good antitumor activity against the Hela cell line with the IC50 value of 36.9 μM, which is better than that of 3b （Z configuration）.展开更多
（R）-1-（4-Methoxyphenyl）propan-2-amine 2a, an optical active intermediate for （R,R）-formoterol, was synthesized from Dalanine in 65% overall yield by using a simple route, which contained protecting amino group, ...（R）-1-（4-Methoxyphenyl）propan-2-amine 2a, an optical active intermediate for （R,R）-formoterol, was synthesized from Dalanine in 65% overall yield by using a simple route, which contained protecting amino group, cyclization, coupling with Grignard reagent, reduction and deprotection.展开更多
5-HT_(1A)receptor is associated with a variety of pathophysiology of neuropsychiatric disorders.Accordingly,we have synthesized a new 5-HT_(1A) receptor ligand(HYNIC-MPP4)and labeled it with^(99m)Tc using N-(2-hydroxy...5-HT_(1A)receptor is associated with a variety of pathophysiology of neuropsychiatric disorders.Accordingly,we have synthesized a new 5-HT_(1A) receptor ligand(HYNIC-MPP4)and labeled it with^(99m)Tc using N-(2-hydroxyethyl)ethylenediaminetriacetic acid(HEDTA)as coligand.^(99m)Tc-HEDTA/HYNIC-MPP4 was prepared under pH 6 at room temperature.Biodistribution of^(99m)Tc-HEDTA/HYNIC-MPP4 in normal mice showed that this complex had moderate brain uptake(0.60%ID·g^(-1)at 2 min p.i.)and good retention.The hippocampus had the highest radioactivity uptake at 2 min p.i.(1.84%ID·g^(-1)).The ratio of Hipp/CB was 3.1 at 2 min p.i.and increased to 4.4 at 60 min p.i.After blocking with 8-hydroxy-2-(dipropylamino)tetralin,the uptake of hippocampus was decreased significantly from 1.84%ID·g^(-1) to 0.53%ID·g^(-1) at 2 min p.i.,while the cerebellum had no significant decrease.This^(99m)Tc complex could be a potent agent for 5-HT_(1A) receptor imaging.展开更多
文摘The two diarylheptanoids (E)-1-(4-hydroxy-3-methoxyphenyl)-7-(4-hydroxyphenyl) hept-4-en-3-one 1 (Gingerenone C) and (±)-5-hydroxy-1-(4-hydroxy-3-methoxyphenyl)-7-(4- hydroxyphenyl)-3-heptanone 2 were synthesized from vanillin 3 and 4-hydroxybenzaldehyde 9.
基金Project supported by the National Natural Science Foundation of China(No.21442014)
文摘The title compound, （E）-1-（7-methoxy-2,2-dimethyl-2,3-dihydrobenzofuran-5-yl）- 3-（2-methoxyphenyl）-2-（1H-1,2,4-triazol-1-yl）propenol （3a）, was synthesized by the Aldol con- densation reaction of 1-（7-methoxy-2,2-dimethyl-2,3-dihydrobenzofuran-5-yl）-2-（1,2,4-triazol- 1-yl）ethanone with 2-methoxybenzaldehyde and then reduced with NaBH4, and its crystal structure was determined by single-crystal X-ray diffraction： monoclinic system, space group P21 with a = 6.2002（3）, b = 12.8452（7）, c = 13.2257（7） ？, Z = 2, V = 1031.23（9） ？3, Mr = 407.46, Dc = 1.312 Mg/m3, S = 1.054, μ = 0.091 mm-1, F（000） = 432, the final R = 0.0353 and wR = 0.0769 for 3161 observed reflections （I 〉 2σ（I））. X-ray analysis displays that the title compound adopts an E configuration for the C（7）=C（8） double bond and S configuration for the chirality center with the specific rotation of –63.75°. Furthermore, the stability of the crystal was maintained through the intermolecular hydrogen bond O（1）–H？？？N（3）. The antitumor assay exhibits that the title compound 3a （E configuration） has a good antitumor activity against the Hela cell line with the IC50 value of 36.9 μM, which is better than that of 3b （Z configuration）.
文摘（R）-1-（4-Methoxyphenyl）propan-2-amine 2a, an optical active intermediate for （R,R）-formoterol, was synthesized from Dalanine in 65% overall yield by using a simple route, which contained protecting amino group, cyclization, coupling with Grignard reagent, reduction and deprotection.
基金Supported by the National Natural Science Foundation of China(Grant No.20401004)the Analysis and Test fund of Beijing Normal University
文摘5-HT_(1A)receptor is associated with a variety of pathophysiology of neuropsychiatric disorders.Accordingly,we have synthesized a new 5-HT_(1A) receptor ligand(HYNIC-MPP4)and labeled it with^(99m)Tc using N-(2-hydroxyethyl)ethylenediaminetriacetic acid(HEDTA)as coligand.^(99m)Tc-HEDTA/HYNIC-MPP4 was prepared under pH 6 at room temperature.Biodistribution of^(99m)Tc-HEDTA/HYNIC-MPP4 in normal mice showed that this complex had moderate brain uptake(0.60%ID·g^(-1)at 2 min p.i.)and good retention.The hippocampus had the highest radioactivity uptake at 2 min p.i.(1.84%ID·g^(-1)).The ratio of Hipp/CB was 3.1 at 2 min p.i.and increased to 4.4 at 60 min p.i.After blocking with 8-hydroxy-2-(dipropylamino)tetralin,the uptake of hippocampus was decreased significantly from 1.84%ID·g^(-1) to 0.53%ID·g^(-1) at 2 min p.i.,while the cerebellum had no significant decrease.This^(99m)Tc complex could be a potent agent for 5-HT_(1A) receptor imaging.
