550358-40-2

Upstream product

• 1484-85-1 3,4-methylenedioxyphenylethylamine 
• 501-53-1 benzyl chloroformate 

Downstream Products

• 550358-42-4 ethyl N-[2-(benzo[1,3]dioxol-5-yl)ethyl]-2-(2,2-dichlorovinyl)-5,6-dimethoxybenzimidate 
• 550358-41-3 N-[2-(benzo[1,3]dioxol-5-yl)ethyl]-2-(2,2-dichlorovinyl)-5,6-dimethoxybenzamide 
• 550358-44-6 ethyl N-[2-(benzo[1,3]dioxol-5-yl)ethyl]-2-ethynyl-5,6-dimethoxybenzimidate 
• 223674-20-2 N-[2-(benzo[1,3]dioxol-5-yl)ethyl]-2-ethynyl-5,6-dimethoxybenzamide 
• 71700-15-7 12b-hydroxy-9,10-dimethoxy-5H-[1,3]dioxolo[4'',5'':4',5']benzo[1',2':4,5]azepino[2,1-a]isoindole-8,13(6H,12bH)-dione 
• 1484-85-1 3,4-methylenedioxyphenylethylamine 

Relevant academic research and scientific papers

Preparation method of aporphine alkaloid

The invention discloses a preparation method of aporphine alkaloid as shown in a formula III. The method comprises the following steps: taking a benzaldehyde compound as shown in a formula III-0 as a raw material, and sequentially carrying out Wittig reaction, Pictet-Spengler reaction, Heck reaction and palladium carbon hydrogen deprotection. A bromine-containing benzaldehyde derivative is selected as a raw material, the carbon-carbon coupling co-production rate and the reaction rate are increased through bromine atoms, and the reaction activity is improved; benzyl chloroformate is adopted for NH protection, and an electron withdrawing group is introduced, so that the reaction yield can be improved; and a styrene methyl ether derivative directly reacts with an acylated phenylethylamine derivative in an acid catalysis system by adopting a one-pot method so as to obtain benzyl tetrahydroisoquinoline. The preparation method has the advantages of mild reaction conditions, low toxicity of used reagents, easily available raw materials, convenient post-treatment and simpler reaction route compared with previous reports, and can be suitable for various reaction substrates.

Aporphine alkaloid derivative as well as preparation method and medical application thereof

The invention discloses an aporphine alkaloid derivative as shown in a formula III, R1 and R2 are respectively and independently selected from alkoxy and methylenedioxy, R3 is selected from H and alkyl, R4 is independently selected from H and alkoxy, but R3 and R4 cannot be H at the same time, or R1 and R2 are methylenedioxy, R3 cannot be H, and R4 cannot be methoxy. The invention further discloses application of the aporphine alkaloid derivative shown in the formula III in preparation of antidepressant drugs. Pharmacological experiments show that the aporphine alkaloid derivative disclosed by the invention has a better anti-depression drug effect, and compared with fluoxetine, the aporphine alkaloid derivative disclosed by the invention has a better anti-depression effect.

Total synthesis of lennoxamine and chilenine via ring-expansion of isoindoloisoquinoline to isoindolobenzazepine

Convenient synthesis of the benzazepine alkaloids, lennoxamine (1) and chilenine (2), is described. The key steps are conversion of methylenelactam (5) to an N-tertiary acyliminium ion precursor (16) and a novel expansion of the six-membered ring of 4 to a benzazepine ring system (3b), which could be transformed into lennoxamine (1) and chilenine (2).