80273-79-6

Basic information

• Product Name: tefludazine
• Synonyms: Lu-18-012
• CAS NO: 80273-79-6
• Molecular Formula: C₂₂H₂₄F₄N₂O
• Molecular Weight: 408.4323728
• Mol File: 80273-79-6.mol
• Article Data: 1

Chemical Properties

• Boiling Point: 476.4°Cat760mmHg
• Flash Point: 241.9°C
• Appearance: /
• Density: 1.285g/cm³
• CAS DataBase Reference: tefludazine(CAS DataBase Reference)
• NIST Chemistry Reference: tefludazine(80273-79-6)
• EPA Substance Registry System: tefludazine(80273-79-6)

Safety Data

• Hazardous Substances Data: 80273-79-6(Hazardous Substances Data)

Upstream product

• 85663-11-2 ethyl 3-<2-bromo-4-(trifluoromethyl)phenyl>-2-cyano-3-(4-fluorophenyl)propanoate 
• 80272-16-8 3-<2-bromo-4-(trifluoromethyl)phenyl>-3-(4-fluorophenyl)propanoic acid 
• 85118-34-9 ethyl 3-<2-bromo-4-(trifluoromethyl)phenyl>-2-cyano-2-propenoate 
• 80272-85-1 3-(4-fluorophenyl)-6-(trifluoromethyl)indan-1-ol 
• 85118-24-7 2-bromo-4-(trifluoromethyl)benzaldehyde 
• 80272-38-4 3-(4-fluorophenyl)-6-(trifluoromethyl)indan-1-one 
• 103-76-4 1-(2-hydroxyethyl)piperazine 
• 85118-26-9 1-chloro-3-(4-fluorophenyl)-6-(trifluoromethyl)indan 

Relevant articles and documents

Neuroleptic activity and dopamine-uptake inhibition in 1-piperazino-3-phenylindans

A series of 1-piperazino-3-phenylindans was synthesized and tested for neuroleptic and thymoleptic activity. Neuroleptic activity was found only in trans racemates and was associated with one of the enantiomers only. The potent and long-acting neuroleptic compound trans-4-[3-(4-fluorophenyl)-6-(trifluoromethyl)indan-1-yl]-1-piperazineeth anol (Lu 18-012, tefludazine) was developed by systematic variation of structural components. Thymoleptic activity was optimized, especially with respect to dopamine-uptake inhibition. No geometrical stereoselectivity was found with regard to dopamine-uptake inhibition, but a high enantioselectivity could be demonstrated for both cis and trans racemates. The most potent compounds were 1-piperazino-3-(3,4-dichlorophenyl)indans with IC50 values of about 2 nM for inhibition of dopamine uptake.