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All total 6 Articles be found
TRICYCLIC PIPERIDINE COMPOUNDS
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, (2016/11/21)
The present invention relates to compounds of the formula (I) wherein R1a, R1b, R2, R3, (R4)n and ring (A) are as described in the description, to their preparation, to pharmaceutically acc
TRICYCLIC PIPERIDINE COMPOUNDS
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, (2015/06/08)
The present invention relates to compounds of the formula (I), wherein R, R1a, R1b, R2, R3, and X are as described in the description, to their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of formula (I), to methods for the preparation of such compounds of formula (I), and especially to their use as TPH modulators.
Enantioselective syntheses of no-carrier-added (n.c.a.) (S)-4-chloro-2-[18F] fluorophenylalanine and (S) - (α-methyl) -4-chloro-2-[18F]fluorophenylalanine
Al-Darwich,Plenevaux,Lemaire,Fiore,Christiaens,Comar,Luxen
, p. 117 - 124 (2007/10/03)
(S)-4-Chloro-2-fluorophenylalanine and (S)-(α-methyl)-4-chloro-2-fluorophenylalanine were synthesized and labeled with no carrier added (n.c.a.) fluorine-18 through a radiochemical synthesis relying on the highly enantioselective reaction between 4-chloro-2-[18F]fluorobenzyl iodide and the lithium enolate of (2S)-1-(tert-butyloxycarbonyl)-2-(tert-butyl)-3-methyl-1,3-imidazolidine-4-one for (S)-4-chloro-2-[18F]fluorophenylalanine and (2S,5S)-1-(tert-butyloxycarbonyl)-2-(tert-butyl)-3,5-dimethyl-1,3-imidazolidine-4-one for (S) - (α-methyl)-4-chloro-2-[18F] fluorophenylalanine. Quantities of about 20-25 mCi were obtained at the end of synthesis, ready for injection after hydrolysis and high performance liquid chromatography (HPLC) purification, with a radiochemical yield of 17%-20% corrected to the end of bombardment after a total synthesis time of 90-105 min from [18F]fluoride. The enantiomeric excesses were shown to be 97% or more for both molecules without chiral separation and the radiochemical and chemical purities were 98% or better.