543741-50-0

Upstream product

• 543741-49-7 (10R,11R)-11-[(2R)-2,3-dihydroxypropyl]-8-fluoro-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-10-yl acetate 
• 98-59-9 p-toluenesulfonyl chloride 
• 887611-88-3 (11Z)-11-{[(4R)-2,2-dimethyl-1,3-dioxolan-4-yl]methylene}-8-fluoro-5,11-dihydro-10H-dibenzo[a,d]cyclohepten-10-one 
• 543741-46-4 (11R)-11-{[(4R)-2,2-dimethyl-1,3-dioxolane-4-yl]methyl}-8-fluoro-5,11-dihydro-10H-dibenzo[a,d]cyclohepten-10-one 
• 890749-72-1 (10R,11R)-11-{[(4R)-2,2-dimethyl-1,3-dioxolan-4-yl]methyl}-8-fluoro-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-10-ol 
• 543741-48-6 (10R,11R)-11-{[(4R)-2,2-dimethyl-1,3-dioxolan-4-yl]methyl}-8-fluoro-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-10-yl acetate 

Relevant academic research and scientific papers

Further improvements of the dibutyl tin oxide-catalyzed regioselective diol tosylation

In this Letter, we report that selective monotosylation of a 1,2-diol is possible using only 0.1 mol % of Bu2SnO. More interestingly, we found that the corresponding tin acetal 3b gave faster conversions and more reproducible reaction times. Moreover, the loading of this catalyst could be as low as 0.05-0.005 mol %.

PROCESS FOR REGIOSELECTIVE DIOL MONO-TOSYLATION USING CATALYTIC AMOUNTS OF A GENERIC DIALKYLTINACETAL

The present invention concerns the use of dibutyl tin oxide for regioselective catalytic diol mono-tosylat ion at a concentration lower than 2 mol%. The present invention also concerns the use of a generic acetal compound of Formula (Ic) in a catalytic process for regioselective diol mono-tosylat ion, wherein Y is selected from the group of C1-6alkyl, phenyl and benzyl. The concentration of the generic acetal compound of Formula (Ic) is less than about 2 mol%, preferably ranges between about 2 mol% and about 0.0005 mol%, preferably ranges between about 0.1 mol% and about 0.005 mol%.

NOVEL SUBSTITUTED TETRACYCLIC TETRAHYDROFURAN, PYRROLIDINE AND TETRAHYDROTHIOPHENE DERIVATIVES

This invention concerns novel substituted tetracyclic tetrahydrofuran, pyrrolidine and tetrahydrothiophene derivatives with binding affinities towards serotonin receptors, in particular 5-HT2A and 5-HT2C receptors, and towards dopamine receptors, in particular dopamine D2 receptors and with norepinephrine reuptake inhibition properties, pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1.

NOVEL SUBSTITUTED TETRACYCLIC TETRAHYDROFURAN, PYRROLIDINE AND TETRAHYDROTHIOPHENE DERIVATIVES AND THEIR USE AS A MEDICAMENT

This invention concerns novel substituted tetracyclic tetrahydrofuran, pyrrolidine and tetrahydrothiophene derivatives with binding affinities towards serotonin receptors, in particular 5-HT2A and 5-HT2C receptors, and towards dopamine receptors, in particular dopamine D2 receptors and with norepinephrine reuptake inhibition properties, pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production. The compounds according to the invention can be represented by general Formula (I), and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1.