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All 10 posts   Subject: what too do   Please login to post   Down

 
    elosejohn
(Stranger)
11-10-04 20:55
No 540904
       what too do     

what would you do with a jar of
1-bis (4-fluorophenyl) methyl piperazine

i guess its ok as is, but is their any  newbee route to a stronger acting synthetic 		 
 
 
 
    Bandil
(The Archetypical "Good Guy")
11-10-04 21:01
No 540905
       Throw it out?     

Throw it out?
Only one way leads to Valhalla - Running amok with TOTAL VIKING POWER 		 
 
 
 
    elosejohn
(Stranger)
11-10-04 21:10
No 540907
       can you tell me why id do this, from my ...     

can you tell me why id do this, from my limited understanding, it should be a great structure to begin with 		 
 
 
 
    Rhodium
(Chief Bee)
11-10-04 23:51
No 540933
User Picture  		      It's not a great structure to begin with, as...     

It's not a great structure to begin with, as it is inactive as is, and none of the substituents can be easily removed.
The Hive - Clandestine Chemists Without Borders 		 
 
 
 
    elosejohn
(Stranger)
11-11-04 00:15
No 540939
       where did you find information on the ...     

where did you find information on the inactivity of this compound i could bearly find any iformation on it in the firstplace


any help would be appreciated 		 
 
 
 
    Rhodium
(Chief Bee)
11-11-04 03:25
No 540960
User Picture  		      Bingo!     

i could bearly find any iformation on it in the first place

That is a very good hint.

If neither the compound itself, nor any substantially similar analogs, are known to be active, it can usually be concluded that it isn't.
The Hive - Clandestine Chemists Without Borders 		 
 
 
 
    elosejohn
(Stranger)
11-11-04 09:01
No 540995
       what makes this inactive compared to other...     

what makes this inactive compared to other piperazines 		 
 
 
 
    Rhodium
(Chief Bee)
11-11-04 09:47
No 541000
User Picture  		      Because it is substituted on both amino ...     

Because it is substituted on both amino groups.
The Hive - Clandestine Chemists Without Borders 		 
 
 
 
    Nicodem
(Hive Bee)
11-11-04 11:47
No 541009
User Picture  		      Bad luck with your compound     

Well, I guess the name you gave to that compound is somewhat misleading for somebees. If using parenthesis correctly it should be 1-[bis(4-fluorophenyl)methyl]piperazine which is used in the synthesis of a vasodilatator drug called flunarizine. If so its structure is:

Molecule: 1-(bis(4-fluorophenyl)methyl)piperazine ("C1CN(CCN1)C(c2ccc(cc2)F)c3ccc(cc3)F")


At first I remembered that this structural element is also incorporated in certain strong DAT ligands but then when I checked the only two related papers I have (DOI:10.1016/S0968-0896(03)00428-0 and  J. Med. Chem. 39(24), 4689-4691) I saw that my memory fooled me as they all have a linker in between the diphenylmethyl and the piperazine moiety. The linker is either –O-(CH2)2- or  -(CH2)3-. A typical example with IC50=2nM for the dopamine transporter is:

Molecule: GBR12909 ("C(c1ccc(cc1)F)(c2ccc(cc2)F)OCCN3CCN(CC3)CCCc4ccccc4")

“The real drug-problem is that we need more and better drugs.” – J. Ott 		 
 
 
 
    Xaja
11-12-04 10:42
       Yup pretty useless alright...
(Rated as: insignificant) 		    
 

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