10214-84-3

Upstream product

• 156-38-7 4-hydroxyphenylacetate 
• 120-20-7 2-(3,4-dimethoxyphenyl)-ethylamine 
• 14199-15-6 Methyl 4-hydroxyphenylacetate 

Downstream Products

• 5884-31-1 2-(4-benzyloxyphenyl)-N-[2-(3,4-dimethoxyphenyl)ethyl]acetamide 
• 52358-58-4 (+/-)-3α,15,16-trimethoxy-8-oxo-Δ^1,6-erythrinan 
• 3195-01-5 L-(-)-N-norarmepavine 
• 1609169-63-2 tert-butyl 1-(4-((5-bromopentyl)oxy)benzyl)-6,7-dimethoxy-3,4-dihydroisoquinoline-2(1H)-carboxylate 
• 1609169-62-1 tert-butyl 1-(4-(4-bromobutoxy)benzyl)-6,7-dimethoxy-3,4-dihydroisoquinoline-2(1H)-carboxylate 
• 1609169-61-0 tert-butyl 1-(4-(3-bromopropoxy)benzyl)-6,7-dimethoxy-3,4-dihydroisoquinoline-2(1H)-carboxylate 
• 1609169-60-9 tert-butyl 1-(4-hydroxybenzyl)-6,7-dimethoxy-3,4-dihydroisoquinoline-2(1H)-carboxylate 
• 1609169-53-0 6,7-dimethoxy-1-(4-((6-(4-phenylpiperidin-1-yl)hexyl)oxy)benzyl)-1,2,3,4-tetrahydroisoquinoline 
• 1609169-59-6 tert-butyl 1-(4-(benzyloxy)benzyl)-6,7-dimethoxy-3,4-dihydroisoquinoline-2(1H)-carboxylate 
• 1609169-52-9 1-(4-((6-(4-benzylpiperazin-1-yl)hexyl)oxy)benzyl)-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline 
• 1609169-51-8 6,7-dimethoxy-1-(4-((6-(4-phenylpiperazin-1-yl)hexyl)oxy)benzyl)-1,2,3,4-tetrahydroisoquinoline 
• 1609169-50-7 4-benzyl-1-(6-(4-((6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolin-1-yl)methyl)phenoxy)hexyl)piperidin-4-ol 
• 1609169-49-4 4-(6-(4-((6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolin-1-yl)methyl)phenoxy)hexyl)morpholine 
• 1609169-48-3 1-(6-(4-((6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolin-1-yl)methyl)phenoxy)hexyl)piperidin-4-ol 

Relevant academic research and scientific papers

Synthesis of the erythrina alkaloid erysotramidine

A concise synthesis of erysotramidine (an alkaloid belonging to the erythrina family) was achieved starting with an inexpensive phenol and amine derivative. The synthesis is based on oxidative phenol dearomatizations mediated by a hypervalent iodine reage

Total Synthesis of (S, S)-Tetramethylmagnolamine via Aerobic Desymmetrization

We describe a concise synthesis of the pseudodimeric tetrahydroisoqunoline alkaloid (S,S)-tetramethylmagnolamine by a catalytic aerobic desymmetrization of phenols. Desymmetrization reactions increase molecular complexity with high levels of efficiency, b

Synthesis and biological evaluation of novel gigantol derivatives as potential agents in prevention of diabetic cataract

As a continuation of our efforts directed towards the development of natural anti-diabetic cataract agents, gigantol was isolated from Herba dendrobii and was found to inhibit both aldose reductase (AR) and inducible nitric oxide synthase (iNOS) activity, which play a significant role in the development and progression of diabetic cataracts. To improve its bioefficacy and facilitate use as a therapeutic agent, gigantol (compound 14f) and a series of novel analogs were designed and synthesized. Analogs were formulated to have different substituents on the phenyl ring (compounds 4, 5, 8, 14a-e), substitute the phenyl ring with a larger steric hindrance ring (compounds 10, 17c) or modify the carbon chain (compounds 17a, 17b, 21, 23, 25). All of the analogs were tested for their effect on AR and iNOS activities and on D-galactose-induced apoptosis in cultured human lens epithelial cells. Compounds 5, 10, 14a, 14b, 14d, 14e, 14f, 17b, 17c, 23, and 25 inhibited AR activity, with IC50 values ranging from 5.02 to 288.8 μM. Compounds 5, 10, 14b, and 14f inhibited iNOS activity with IC50 ranging from 432.6 to 1188.7 μM. Compounds 5, 8, 10, 14b, 14f, and 17c protected the cells from D-galactose induced apoptosis with viability ranging from 55.2 to 76.26%. Of gigantol and its analogs, compound 10 showed the greatest bioefficacy and is warranted to be developed as a therapeutic agent for diabetic cataracts.

Effect of 1-Substitution on Tetrahydroisoquinolines as Selective Antagonists for the Orexin-1 Receptor

Selective blockade of the orexin-1 receptor (OX1) has been suggested as a potential approach to drug addiction therapy because of its role in modulating the brain's reward system. We have recently reported a series of tetrahydroisoquinoline-based OX1 selective antagonists. Aimed at elucidating structure-activity relationship requirements in other regions of the molecule and further enhancing OX1 potency and selectivity, we have designed and synthesized a series of analogues bearing a variety of substituents at the 1-position of the tetrahydroisoquinoline. The results show that an optimally substituted benzyl group is required for activity at the OX1 receptor. Several compounds with improved potency and/or selectivity have been identified. When combined with structural modifications that were previously found to improve selectivity, we have identified compound 73 (RTIOX-251) with an apparent dissociation constant (Ke) of 16.1 nM at the OX1 receptor and >620-fold selectivity over the OX2 receptor. In vivo, compound 73 was shown to block the development of locomotor sensitization to cocaine in rats. (Chemical Equation Presented).

Design, synthesis and biological evaluation of benzylisoquinoline derivatives as multifunctional agents against Alzheimer's disease

A novel series of benzylisoquinoline derivatives were designed, synthesized, and evaluated as multifunctional agents against Alzheimer's disease (AD). The screening results showed that most of the compounds significantly inhibited cholinesterases (ChEs),

Total synthesis of new 8-(arylmethyl)berbines

The total synthesis of the natural compound (8S*, 14S*)-8-(4'hydroxybenzyl)-2,3-dimethoxyberbin-10-ol and its C-8 epimer has been conveniently developed by making use of the diastereoselective Stevens rearrangement of the corresponding N-(arylmethyl)berbi

Method and health food for preventing and/or alleviating psychiatric disorder, and/or for effectuating sedation

A method for preventing and/or alleviating a psychiatric disorder, and/or effectuating sedation, comprising administering a benzylisoquinoline derivative represented by General Formula (I): wherein R1, R2, R3 and X each re