94460-54-5

Upstream product

• 64881-05-6 1-<4-(benzyloxy)-3-methoxyphenyl>ethan-2-ol 
• 100-44-7 benzyl chloride 
• 21473-46-1 2-(4'-benzyloxy-3'-methoxyphenyl)-1-nitroethane 
• 29973-91-9 4-benzyloxy-3-methoxyphenylacetic acid 
• 121-33-5 vanillin 
• 100-39-0 benzyl bromide 
• 63909-38-6 3-methoxy-4-benzyloxy-ω-nitrostyrolene 
• 16209-54-4 methyl 4-benzyloxy-3-methoxyphenylethanoate 
• 55708-65-1 1-(benzyloxy)-4-ethenyl-2-methoxybenzene 
• 2426-87-1 3-methoxy-4-(phenylmethoxy)benzaldehyde 

Downstream Products

• 912957-28-9 Viscolin 
• 918549-42-5 1-Benzyloxy-4-[(Z)-3-(4-benzyloxy-3-methoxy-phenyl)-propenyl]-2,3,5-trimethoxy-benzene 
• 634893-23-5 [1-ethyl-3-[3-methoxy-4-(4-phenyl-butoxy)-phenyl]-1-(3-oxo-1,5-dihydro-3λ⁵-benzo[e][1,3,2]dioxaphosphepin-3-yloxymethyl)-propyl]-carbamic acid tert-butyl ester 
• 463952-31-0 [3-[3-methoxy-4-(4-phenyl-butoxy)-phenyl]-1-methyl-1-(3-oxo-1,5-dihydro-3λ⁵-benzo[e][1,3,2]dioxaphosphepin-3-yloxymethyl)-propyl]-carbamic acid tert-butyl ester 
• 463952-32-1 {3-[3-methoxy-4-(4-phenyl-butoxy)-phenyl]-1-methyl-1-phosphonooxymethyl-propyl}-carbamic acid tert-butyl ester 
• 634893-19-9 {1-ethyl-1-hydroxymethyl-3-[3-methoxy-4-(4-phenyl-butoxy)-phenyl]-propyl}-carbamic acid tert-butyl ester 
• 634893-08-6 (2R,5R)-2-[2-(4-benzyloxy-3-methoxyphenyl)ethyl]-3,6-diethoxy-2-ethyl-5-isopropyl-2,5-dihydropyrazine 
• 463952-30-9 {1-hydroxymethyl-3-[3-methoxy-4-(4-phenyl-butoxy)-phenyl]-1-methyl-propyl}-carbamic acid tert-butyl ester 
• 634893-07-5 (2R,5R)-2-[2-(4-Benzyloxy-3-methoxy-phenyl)-ethyl]-3,6-diethoxy-5-isopropyl-2-methyl-2,5-dihydro-pyrazine 
• 634893-16-6 [3-(4-benzyloxy-3-methoxy-phenyl)-1-ethyl-1-hydroxymethyl-propyl]-carbamic acid tert-butyl ester 
• 634893-15-5 [3-(4-benzyloxy-3-methoxy-phenyl)-1-hydroxymethyl-1-methyl-propyl]-carbamic acid tert-butyl ester 

Relevant academic research and scientific papers

Benzo aza compound, preparation method and use thereof

Belonging to the field of pharmaceutical chemistry, the invention relates to a benzoazepine compound, a preparation method and application thereof, in particular to the benzoazepine compound, its preparation method and application in the field of treatment of nervous system diseases, especially application in the field of drug addiction related to dopamine D1 and D3 receptors. The benzoazepine compound and pharmacologically acceptable inorganic or organic salts thereof have a structure shown as formula (I). Results of drug experiments carried out by the invention show that the benzoazepine compound and its pharmacologically acceptable inorganic or organic salts have high antagonistic activity on dopamine D1 and D3, can be used as drug leads for further development of dopamine receptor antagonists with good selectivity and high activity, and can be used as potential drugs for treatment of drug addiction by dopamine D1, D3 receptor antagonists. (formula (I)).

Functional reversal of (?)-Stepholidine analogues by replacement of benzazepine substructure using the ring-expansion strategy

(?)-Stepholidine is an active ingredient of the Chinese herb Stephania and naturally occurring tetrahydroprotoberberine alkaloid with mixed dopamine receptor D1 agonistic and dopamine receptor D2 antagonistic activities. In this work, a series of novel hexahydrobenzo[4,5]azepino [2,1-a]isoquinolines were designed and synthesized as ring-expanded analogues of (?)-Stepholidine. Initial pharmacological assays demonstrated that a benzazepine replacement was associated with significant increase in selectivity and functional reversal at dopamine receptor D1. Compound-(?)-15e (Ki?=?5.32?±?0.01?nm) is more potent than (?)-Stepholidine (Ki?=?13?nm) and was identified as a selective dopamine receptor D1 antagonist (IC50?=?0.14?μm). Moreover, molecular modeling suggested that (?)-15e might exert its dopamine receptor D1 antagonistic activities through interacting with the transmembrane helix 7 of dopamine receptor D1.

Total synthesis and biological evaluation of viscolin, a 1,3-diphenylpropane as a novel potent anti-inflammatory agent

Total synthesis of viscolin, an anti-inflammatory 1,3-diphenylpropane isolated from Viscum coloratum, employing the Wittig reaction is reported. Key steps in the synthesis of viscolin depend on the selection of protecting groups to maintain the para hydroxyl group that is the most critical chemical structure influencing the biological activity of viscolin and the utilization of microwave-assisted Wittig olefination reaction. Anti-inflammatory potency of the synthetic viscolin, its precursor product 16, and its analogue 17, through their effects on reactive oxygen species (ROS), nitric oxide (NO), and pro-inflammatory cytokine production in leukocytes and microglial cells were evaluated. Excellent inhibition of ROS and NO production in inflammatory cells could confer the synthetic viscolin to be a potent anti-inflammatory agent for the treatment of oxidative stress-induced diseases.