Synthesis and biological evaluation of a new series of phenothiazine- containing protein farnesyltransferase inhibitors
Two new families of human farnesyltransferase inhibitors 13a-m and 14a-d, based on a phenothiazine scaffold, were synthesized. Compounds 14a and 14b were the most promising inhibitors of human farnesyltransferase with IC50 values of 0.7 and 0.6 μM, respectively.
Abuhaie, Cristina-Maria,Ghinet, Alina,Farce, Amaury,Dubois, Joelle,Gautret, Philippe,Rigo, Benoit,Belei, Dalila,Bicu, Elena
p. 101 - 110
(2013/03/13)
PROCESS FOR THE PREPARATION OF A PYRAZOLE DERIVATIVE
Disclosed here is a process for the preparation of 3 - amino pyrazole derivative of Formula (I) where R1 = H, C1 - C4 alkyl group or benzyl group or phenyl group; R2 = C1 - C6 alkyl group or benzyl group; comprising a step of reacting the compound of Formula (Ill) with hydrazine hydrate.
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Page/Page column 7
(2011/06/23)
Reaction of Ortho Esters with Secondary Amines
The scope of the reaction of ortho esters with secondary amines has been explored.With p-toluenesulfonic acid as catalyst, N-alkylanilines and orthoformates gave high yields of N-alkylformanilides and N,N-dialkylanilines in contrast to previous work with other acid catalysts where ortho amides were produced in low yield.Aliphatic cyclic amines (e.g., morpholine, piperidine) and orthoformates gave the corresponding ortho amides.This constitutes a new convenient synthesis of these useful reagents.
Swaringen, Roy A.,Eaddy, John F.,Henderson, Thomas R.
p. 3986 - 3989
(2007/10/02)
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