- PROCESS FOR PREPARATION OF TRICLABENDAZOLE
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The present invention discloses a method for preparing Triclabendazole comprising condensing N-(4,5-dichloro-2-ni-trophenyl)acetamide with 2,3-dichlorophenol to obtain 4-chloro-5(2,3-dichlorophenoxy)-2-nitrophenyl acetamide and it to obtain 4-chloro-5(2,3-dichlorophenoxy)-2-nitroaniline; reducing 4-chloro-5(2,3-dichlorophenoxy)-2-nitroaniline in presence of Raney nickel to obtain 4-chloro-5-(2,3-dichlorophenoxy)benzene-1,2-diamine of; cyclising 4-chloro-5-(2,3-dichlorophenoxy)benzene-1,2-diamine in presence of carbondisulfide to obtain 6-chloro-5-(2,3-dichlorophenoxy)-1H-benzimidazole-2-thiol; methylating 6-chloro-5-(2,3-dichlorophenoxy)-1H-benzimidazole-2-thiol using a methylating agent to obtain triclabendazole methanesulfonate salt; converting triclabendazole methanesulfonate salt to hydrochloride salt of Triclabendazole and hydrolysing it to obtain Triclabendazole.
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Paragraph 0024
(2013/11/19)
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- PROCESS FOR PREPARATION OF TRICLABENDAZOLE
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The present invention discloses a method for preparing Triclabendazole comprising condensing N-(4,5-dichloro-2-nitrophenyl)acetamide with 2,3-dichlorophenol to obtain 4-chloro-5(2,3-dichlorophenoxy)-2-nitrophenyl acetamide and it to obtain 4- chloro-5(2,3-dichlorophenoxy)-2-nitroaniline; reducing 4-chloro-5(2,3- dichlorophenoxy)-2-nitroaniline in presence of Raney nickel to obtain 4-chloro-5- (2,3-dichlorophenoxy)benzene-l,2-diamine of; cyclising 4-chloro-5-(2,3- dichlorophenoxy)benzene-l,2-diamine in presence of carbondisulfide to obtain 6- chloro-5-(2,3-dichlorophenoxy)-lH-benzimidazole-2-thiol; methylating 6-chloro-5- (2,3-dichlorophenoxy)-lH-benzimidazole-2 -thiol using a methylating agent to obtain triclabendazole methanesulfonate salt; converting triclabendazole methanesulfonate salt to hydrochloride salt of Triclabendazole and hydrolysing it to obtain Triclabendazole.
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Page/Page column 6
(2012/06/15)
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- Synthesis and biological activity of 2-(trifluoromethyl)-1H-benzimidazole derivatives against some protozoa and Trichinella spiralis
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A series of 2-(trifluoromethyl)-1H-benzimidazole derivatives (1ae1i) were synthesized via Phillips cyclocondensation of a substituted 1,2-phenylenediamine and trifluoroacetic acid. The synthesized compounds were evaluated in vitro against various protozoan parasites: Giardia intestinalis, Entamoeba histolytica, Trichomonas vaginalis and Leishmania mexicana, and they showed nanomolar activities against the first three protozoa tested. The compounds were also tested in vitro and in vivo against the nematode Trichinella spiralis. Compounds 1b, 1c and 1e had the most desirable in vitro antiparasitic profile against all parasites studied. In the in vivo model against T. spiralis, compounds 1b and 1e showed good activity against the adult phase at 75 mg/Kg. However, against the muscle larvae stage, only compound 1f exhibited in vivo antiparasitic efficacy.
- Hernández-Luis, Francisco,Hernández-Campos, Alicia,Castillo, Rafael,Navarrete-Vázquez, Gabriel,Soria-Arteche, Olivia,Hernández-Hernández, Manuel,Yépez-Mulia, Lilián
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experimental part
p. 3135 - 3141
(2010/09/03)
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- Microbicidal benzotriazole compounds
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Novel benzotriazolesulfonic acid derivatives of formula STR1 wherein: R1 is hydrogen, halogen, C1 -C4 alkyl, C1 -C4 alkoxy, C1 -C4 haloalkoxy having at least two identical or different halogen atoms, CF3, nitro or the group N(R')R", wherein R' and R" are each independently of the other C1 -C4 alkyl; R2 is phenoxy or phenylthio each of which is unsubstituted or mono- to tri-substituted by halogen, C1 -C4 alkyl, C1 -C4 alkoxy, C1 -C4 haloalkoxy having at least two identical or different halogen atoms, cyano, nitro, C2 -C4 alkenyl, C2 -C4 alkynyl, phenyl, 2-phenylethynyl or by a further phenoxy radical that is unsubstituted or substituted by halogen, C1 -C4 alkyl and/or by C1 -C4 alkoxy; or R2 is the radical O--CH2 --O; R3 is alkyl, aryl or aralkyl having a maximum of 14 carbon atoms, these radicals can be substituted by halogen, C1 -C4 alkyl and/or by nitro; including the position isomers of R1 and R2, insofar as those substituents occupy positions 5 and 6. The novel compounds have plant-protecting properties and are suitable especially for protecting plants against attack by phytopathogenic microorganisms such as fungi, especially Oomycetes.
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