163339-71-7

Upstream product

• 3218-49-3 3,4-dichloro-benzeneacetonitrile 
• 6725-44-6 methyl 2-(3,4-dichlorophenyl)acetate 

Downstream Products

• 334477-10-0 3-(3,4-dichloro-phenyl)-piperazin-2-one 
• 877397-17-6 1-(3,4-dichlorophenyl)-1,2-cyclopropane-dicarboxylic acid dimethyl ester 
• 410074-74-7 (±)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane hydrochloride 
• 410074-74-7 Amitifadine hydrochloride 
• 344245-65-4 1-(3,4-dichlorophenyl)-1,2-cyclopropanedicarboxylic acid 
• 66504-44-7 (±)-1-(3,4 dichlorophenyl)-3-azabicyclo[3.1.0]-hexane-2,4-dione 
• 86215-36-3 (+/-)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0.]hexane hydrochloride 
• 1186200-70-3 C₁₁H₁₀Cl₂O₃S 
• 207404-79-3 [2-(4-{2-[2-(3,4-dichloro-phenyl)-4-(3,5-dimethyl-benzoyl)-piperazin-1-yl]-2-oxo-ethylamino}-piperidin-1-yl)-1-(1H-indol-3-ylmethyl)-2-oxo-ethyl]-carbamic acid tert-butyl ester 
• 207404-76-0 [(S)-2-(4-{2-[(R)-2-(3,4-Dichloro-phenyl)-4-(3,5-dimethyl-benzoyl)-piperazin-1-yl]-2-oxo-ethylamino}-piperidin-1-yl)-1-(4-hydroxy-benzyl)-2-oxo-ethyl]-carbamic acid tert-butyl ester 
• 207404-75-9 [(S)-1-Benzyl-2-(4-{2-[(R)-2-(3,4-dichloro-phenyl)-4-(3,5-dimethyl-benzoyl)-piperazin-1-yl]-2-oxo-ethylamino}-piperidin-1-yl)-2-oxo-ethyl]-carbamic acid tert-butyl ester 
• 207404-82-8 [(R)-1-Benzyl-2-(4-{2-[(R)-2-(3,4-dichloro-phenyl)-4-(3,5-dimethyl-benzoyl)-piperazin-1-yl]-2-oxo-ethylamino}-piperidin-1-yl)-2-oxo-ethyl]-carbamic acid tert-butyl ester 
• 207404-77-1 [(S)-2-(4-{2-[(R)-2-(3,4-Dichloro-phenyl)-4-(3,5-dimethyl-benzoyl)-piperazin-1-yl]-2-oxo-ethylamino}-piperidin-1-yl)-2-oxo-1-phenyl-ethyl]-carbamic acid tert-butyl ester 
• 207404-83-9 [(R)-2-(4-{2-[(R)-2-(3,4-Dichloro-phenyl)-4-(3,5-dimethyl-benzoyl)-piperazin-1-yl]-2-oxo-ethylamino}-piperidin-1-yl)-2-oxo-1-phenyl-ethyl]-carbamic acid tert-butyl ester 

Relevant academic research and scientific papers

USE OF AMITIFADINE, (+)-1-(3,4-DICHLOROPHENYL)-3-AZABICYCLO[3.1.0]HEXANE IN METHODS AND COMPOSITIONS WITH ENHANCED EFFICACY AND REDUCED METABOLIC SIDE EFFECTS AND TOXICITY FOR TREATMENT OF DEPRESSION AND OTHER CENTRAL NERVOUS SYSTEM DISORDERS AND CONDITIO

The present invention relates to (+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane and pharmaceutically acceptable active salts, polymorphs, glycosylated derivatives, metabolites, solvates, hydrates, and/or prodrugs of (+)-1-(3,4-dichlorophenyl)-3-azab

PREPARATION AND USE OF (+)-1-(3,4-DICHLOROPHENYL)-3-AZABICYCLO[3.1.0]HEXANE IN THE TREATMENT OF CONDITIONS AFFECTED BY MONOAMINE NEUROTRANSMITTERS

The present invention relates to (+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane and pharmaceutically acceptable active salts, polymorphs, glycosylated derivatives, metabolites, solvates, hydrates, and/or prodrugs of (+)-1-(3,4-dichlorophenyl)-3-azab

PROCESS FOR PRODUCTION OF THIOPHENE COMPOUND AND INTERMEDIATE THEREOF

To provide a novel process for producing a 2-aryl-3-hydroxy-4-substituted carbonyl thiophene compound or an intermediate thereof useful as an intermediate for production of medicines and agricultural chemicals. A 2-aryl acetate compound represented by the formula (1): wherein R1 is an aryl group or the like, R4 is a C1-3 alkyl group or the like, and X is a leaving group, is reacted with a thioacetic acid compound to form a thioacetyl compound (3), the thioacetyl compound (3) is reacted with a vinyl ketone compound to form a γ-ketosulfide compound (5), which is cyclized under basic conditions to form a dihydrothiophene compound (6), and the dihydrothiophene compound (6) is oxidized by using an oxidizing agent to produce a 2-aryl-3-hydroxy-4-substituted carbonyl thiophene compound (7).

Novel polymorphs of azabicyclohexane

The invention provides polymorphic crystalline forms of acid addition salts of (+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane designated as polymorph form A, polymorph form B and polymorph form C, where polymorph form A is more thermodynamically stable than the other forms, methods for preparing and using such polymorph forms and pharmaceutical compositions containing such polymorph forms.

NOVEL POLYMORPHS OF AZABICYCLOHEXANE

The invention provides polymorphic crystalline forms of acid addition salts of (+)-1-(3, 4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane designated as polymorph form A, polymorph form B and polymorph form C, where polymorph form A is more thermodynamically stable than the other forms, methods for preparing and using such polymorph forms and pharmaceutical compositions containing such polymorph forms.

Synthesis and NK1/NK2 binding activities of a series of diacyl-substituted 2-arylpiperazines

The synthesis and binding affinity for hNK1 and hNK2 receptors of a series of diacyl substituted 2-aryl piperazines are described. SAR evaluation led to the racemic derivative 11g as an apparent dual inhibitor. Chiral chromatographic separation of 11g led to the observation that NK1 activity was shown by one enantiomer (13a) and NK2 activity was shown by the other enantiomer (13b). X-ray crystallographic analysis of the crystalline di-BOC derivative of the NK2 active piperazine (15) showed that the 2R configuration was associated with NK2 activity. Further derivatization indicated that dual NK1/NK2 activity could be built into the 2R series.