- TRICYCLIC PIPERIDINE COMPOUNDS
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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
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- TRICYCLIC IMIDAZOLE COMPOUNDS AS INHIBITORS OF TRYPTOPHAN HYDROXYLASE
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The present invention relates to compounds of the formula (I), wherein R1a, R1b, R2, R3, and X are as described in the description, to their preparation, to pharmaceutically acceptable salts thereof, and to thei
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- TRICYCLIC PIPERIDINE COMPOUNDS
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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.
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- Enantioselective syntheses of no-carrier-added (n.c.a.) (S)-4-chloro-2-[18F] fluorophenylalanine and (S) - (α-methyl) -4-chloro-2-[18F]fluorophenylalanine
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(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.
- Al-Darwich,Plenevaux,Lemaire,Fiore,Christiaens,Comar,Luxen
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p. 117 - 124
(2007/10/03)
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- Heterocyclic pesticidal compounds
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Compounds of the formula (I) STR1 which contain between 10 and 27 carbon atoms, and wherein m and n are independently selected from 0, 1 and 2; R2a is hydrogen, methyl, or ethyl; R2b is acetylene or contains between 3 and 18 carbon atoms and is a group R7, wherein R7 is a C1-13 non-aromatic hydrocarbyl group, optionally substituted by a cyano or C1-4 carbalkoxy group and/or by one or two hydroxy groups and/or by one to five halo atoms which are the same or different and/or by one to three groups R8 which are the same or different and each contain one to four hetero atoms, which are the same or different and are chosen from oxygen, sulphur, nitrogen and silicon, 1 to 10 carbon atoms and optionally 1 to 6 fluoro or chloro atoms or R2b is a 6-membered aromatic ring substituted by cyano and/or by one to three groups R8 and/or by a group --C CH, --C C-R7 or C C-halo and/or by one to five halo atoms and/or by one to three C1-4 haloalkyl groups wherein R7 and R8 are as hereinbefore defined; R4 and R6 are the same or different and are chosen from hydrogen, methyl, trifluoromethyl or cyano; and R5 is hydrogen or methyl provided that R2b is not propyl or butyl are described which have pesticidal activity, particularly against arthropod pests. Pesticidal formulations containing the compounds of the formula (I), their use in the control of pests and method for their preparation are also disclosed.
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- 'HALEX' FLUORINATION OF CHLORINATED BENZALDEHYDES AND BENZOYL CHLORIDES
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Spray-dried potassium fluoride, suspended in sulpholane at 220 degC, converted 2,4- and 2,6-dichlorobenzaldehyde into the corresponding difluoroaldehydes (yields ca. 65percent).Small amounts of the mono-substituted products (2-chloro-4-fluoro- + 4-chloro-2-fluorobenzaldehyde, and 2-chloro-6-fluoro-benzaldehyde, respectively) were also produced.Similar treatment of the 3,4-dichloro-analogue gave 3-chloro-4-fluorobenzaldehyde (yield 98percent, conversion 68percent), but 2- and 4-chlorobenzaldehyde gave very poor yields (ca. 5percent) of the 2- and 4-fluoro-derivatives. 2-Fluoro-, 4-fluoro- and 3-chloro-4-fluorobenzoyl fluoride were obtained (yields 60-65percent) by heating the corresponding chlorobenzoyl chlorides with potassium fluoride in sulpholane.
- Banks, R. Eric,Mothersdale, Kevin N.,Tipping, Anthony E.,Tsiliopoulos, Efthimios,Cozens, Barry J.,et al.
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p. 529 - 537
(2007/10/02)
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