Facile Synthesis of 5-Carboxylate Substituted Piperazin-2-ones as Peptidomimetic Agents.
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چکیده
منابع مشابه
Synthesis of novel 2-(substituted amino)alkylthiopyrimidin-4(3H)-ones as potential antimicrobial agents.
5-Alkyl-6-(substituted benzyl)-2-thiouracils 3a,c were reacted with (2-chloroethyl) diethylamine hydrochloride to afford the corresponding 2-(2-diethylamino)ethylthiopyrimidin- 4(3H)-ones 4a,b. Reaction of 3a-c with N-(2-chloroethyl)pyrrolidine hydrochloride and/or N-(2-chloroethyl)piperidine hydrochloride gave the corresponding 2-[2-(pyrrolidin-1-yl)ethyl]-thiopyrimidin-4(3H)-ones 5a-c and 2-[...
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Enantiomerically-enriched trichloromethyl-containing alcohols, obtained by asymmetric reduction, can be transformed regioselectively into 1-substituted piperazinones by modified Jocic reactions with little or no loss of stereochemical integrity. This methodology can be easily used to synthesise important pharmaceutical compounds such as the fluorobenzyl intermediate of a known PGGTase-I inhibitor.
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A wide variety of titled compounds, several of which have neuro-protecting properties has been prepared in yields ranging between 70 to 90%. The compounds were identified by 1 HNMR, 13 C NMR, 1D and 2D NOE analysis, and HRMS. An investigation of the effect of certain 5-substitutuents on the E to Z ratios in DMSO-d6 was carried out. The 5nitro and 5-acetyl substituents were not isomerized, where...
متن کاملFacile one-pot synthesis of 5-substituted hydantoins.
5-Substituted and 5,5-disubstituted hydantoins are synthesised from the corresponding aldehydes or ketones, using a one-pot, gallium(III) triflate-catalysed procedure that is compatible with a range of substrates and solvents.
متن کامل5-sulfosalicylic acid as an efficient organocatalyst for environmentally benign synthesis of 2-substituted benzimidazoles
A water soluble, Bronsted acid, 5-sulfosalicylic acid as an efficient organocatalyst was used for the synthesis of physiologically active 2-substituted benzimidazole derivatives from o-phenylenediamine and aromatic aldehydes in ethanol at reflux condition. Cost-effectiveness, use of non-hazardous solvents, metal free and commercially available catalyst, single-step, environmentally fri...
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ژورنال
عنوان ژورنال: ChemInform
سال: 2003
ISSN: 0931-7597,1522-2667
DOI: 10.1002/chin.200312151