329966-21-4

Upstream product

• 934-00-9 3-methocycatechol 
• 113826-06-5 (R)-glycidyl tosylate 
• 98-59-9 p-toluenesulfonyl chloride 
• 329966-19-0 (2S)-3-(2,3-dihydroxyphenoxy)-1,2-bis(tosyloxy)propane 
• 329966-18-9 (2S)-3-(2,3-dimethoxyphenoxy)-1,2-bis(tosyloxy)propane 
• 329966-16-7 (2S)-3-(2,3-dimethoxyphenoxy)-1,2-propanediol acetonide 
• 329966-17-8 (2R)-3-(2,3-dimethoxyphenoxy)-1,2-propanediol 
• 5150-42-5 2,3-dimethoxyphenol 
• 678992-70-6 (R)-2-(2-Benzyloxy-3-methoxy-phenoxymethyl)-oxirane 
• 122450-20-8 2-benzyloxy-3-methoxyphenol 
• 2011-06-5 2-benzyloxy-3-methoxybenzaldehyde 
• 24677-78-9 2,3-dihydroxybenzaldehyde 
• 86734-60-3 2-(benzyloxy)-3-hydroxybenzaldehyde 
• 145167-53-9 (S)-8-methoxy-1,4-benzodioxane-2-methanol 

Downstream Products

• 766498-48-0 (2S)-2-[((2-(2,6-dimethoxyphenoxy)ethyl)amino)methyl]-8-methoxy-1,4-benzodioxane 

Relevant academic research and scientific papers

Novel, broad-spectrum anticonvulsants containing a sulfamide group: Pharmacological properties of (S)- N -[(6-chloro-2,3-dihydrobenzo[1,4]dioxin-2- yl)methyl]sulfamide (JNJ-26489112)

Broad-spectrum anticonvulsants are of considerable interest as antiepileptic drugs, especially because of their potential for treating refractory patients. Such "neurostabilizers" have also been used to treat other neurological disorders, including migraine, bipolar disorder, and neuropathic pain. We synthesized a series of sulfamide derivatives (4-9, 10a-i, 11a, 11b, 12) and evaluated their anticonvulsant activity. Thus, we identified promising sulfamide 4 (JNJ-26489112) and explored its pharmacological properties. Compound 4 exhibited excellent anticonvulsant activity in rodents against audiogenic, electrically induced, and chemically induced seizures. Mechanistically, 4 inhibited voltage-gated Na+ channels and N-type Ca2+ channels and was effective as a K+ channel opener. The anticonvulsant profile of 4 suggests that it may be useful for treating multiple forms of epilepsy (generalized tonic-clonic, complex partial, absence seizures), including refractory (or pharmacoresistant) epilepsy, at dose levels that confer a good safety margin. On the basis of its pharmacology and other favorable characteristics, 4 was advanced into human clinical studies.

Modulation of selective serotonin reuptake inhibitor and 5-HT1A antagonist activity in 8-aza-bicyclo[3.2.1]octane derivatives of 2,3-dihydro-1,4-benzodioxane

2,3-Dihydro-1,4-benzodioxanes with aryl 8-aza-bicyclo[3.2.1]oct-3-ene attachments 2 produce compounds with potent 5-HT-T affinity, and weak 5-HT 1A affinity and α1 affinity. This compares with 2,3-dihydro-1,4-benzodioxanes containing 8-aza-bicyclo[3.2.1] octan-3-ol attachments 4 which possess potent 5-HT1A affinity, moderate to good selectivity over α1 and little 5-HT-T affinity. A 3-benzothiophene analogue of 4 (30) was synthesized which possesses potent 5-HT1A affinity and especially good selectivity over both α1 and 5-HT-T.

8-azabicyclo[3.2.1] octane-3-methanamine derivatives as ligands of D2 and D3 dopamine and 5HT1A and 5HT2 serotonin receptors

Compounds of general formula (I) in which U represents a group of general formula (A) or (B) in which formulae V represents a hydrogen or halogen atom, a (C1-C3)alkyl group or one or two (C1-C3)alkoxy groups, W and X each represent, respectively, either two oxygen atoms, or an oxygen atom and a CH2group, or a CH2group and an oxygen atom, or an oxygen atom and a CO group, n represents the number 0 or 1, R represents either a propyl group when U represents a group of general formula (A), or a hydrogen atom or a (C1-C3)alkyl group when U represents a group of general formula (B), Y represents one or more atoms or groups chosen from the following: hydrogen, halogen, (C1-C3)alkyl and (C1-C3)alkoxy, Z represents two hydrogen atoms or an oxygen atom.