- A new enantioselective synthesis of the anti-Parkinson agent safinamide
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An alternative highly enantioselective synthesis of the anti-Parkinson agent safinamide from simple, commercially available, starting materials is described. The protocol might also be useful in the synthesis of structural variants of safinamide, such as ralfinamide or related analogues. Georg Thieme Verlag Stuttgart New York.
- Reddi, Anjaneyulu,Mujahid, Mohammad,Sasikumar, Murugesan,Muthukrishnan, Murugan
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p. 1751 - 1756
(2014/07/08)
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- AN IMPROVED SYNTHESIS OF ANTI-PARKINSON AGENT
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The present invention relates to an improved process for synthesis of anti-Parkinson compound of formula (I) from commercially available (R)-benzyl glycidyl ether, wherein the compound obtained has enantiopurity greater than >98%. Formula (I) wherein R1 and R2 are each independently selected from hydrogen or halogen.
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Page/Page column 15-16
(2014/11/13)
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- Antitumor agents. 120. New 4-substituted benzylamine and benzyl ether derivatives of 4'-O-demethylepipodophyollotoxin as potent inhibitors of human DNA topoisomerase II
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A number of new 4'-O-demethylepipodophyllotoxin derivatives possessing various 4β-N- or 4β-O-benzyl groups have been synthesized and evaluated for their inhibitory activity against the human DNA topoisomerase II as well as for their activity in causing cellular protein-linked DNA breakage. The 4β-N-benzyl derivatives 9-22 are, in general, as active or more active than etoposide (1). The most active compounds are 14, 16, and 17, which are more than 2-fold more potent than 1. The results indicated that a basic unsubstituted 4β-benzylamino moiety is structurally required for the enhanced activity. Replacement of the benzyl nitrogen with oxygen gave compounds (23 and 24) which are inactive. The ability of these compounds to inhibit human DNA topoisomerase II and to cause protein-linked DNA breakage appears to have no direct correlation with cytotoxicity in KB cells.
- Zhou,Wang,Chang,Chen,Cheng,Lee
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p. 3346 - 3350
(2007/10/02)
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- Carbon-Halogen Bonding Studies. Halogen Redistribution Reactions between Alkyl or Acetyl Halides and Tri-n-butyltin Halides
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The equilibrium positions have been determined for the halogen redistribution reactions of tri-n-butyltin halides with a variety of structurally different types of alkyl halides and with acetyl halides.These have been related through the reaction ΔGo values to carbon-halogen bond dissociation energy differences.It is suggested that the trends observed in the latter may provide evidence for the existence of a small steric bond weakening effect in the order C-I > C-Br > C-Cl bonds on going from methyl to primary, secondary, and tertiary alkyl halides.On the other hand, with the 2,3-? bond containing allyl, benzyl, and propargyl halides , α-haloacetones, and haloacetonitriles, there may be some type of electronic carbon-halogen bond strengthening effect which lies in order C-I > C-Br > C-Cl.Finally, for the acetyl halides, the data are in agreement with increases in bond strengths resulting from ? contributions being in the order C-Cl > C-Br > C-I.
- Friedrich, Edwin C.,Abma, Charles B.
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p. 1367 - 1371
(2007/10/02)
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