- Iron-catalyzed reaction of urea with alcohols and amines: A safe alternative for the synthesis of primary carbamates
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A general study of the iron-catalyzed reaction of urea with nucleophiles is here presented. The carbamoylation of alcohols allows for the synthesis of N-unsubstituted (primary) carbamates, including present drugs (Felbamate and Meprobamat, without the necessity to apply phosgene and related derivatives. Using amines as nucleophiles gave rise to the respective mono-and disubstituted ureas via selective transamidation reaction. These atom-economical transformations provide a direct and selective access to valuable compounds from cheap and readily available urea using a simple Lewis-acidic iron(Icatalyst.
- Pe?a-López, Miguel,Neumann, Helfried,Beller, Matthias
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p. 2233 - 2238
(2017/07/25)
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- Benzo-as-triazine derivatives
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The invention relates to new benzo-as-triazine derivatives of the formulae (I) and (Ia) and pharmaceutically acceptable acid addition salts thereof, STR1 wherein R1 and R2 each represent hydrogen, a C1-20 alkylcarbonyl group, a phenylcarbonyl or phenyl-(C1-4 alkyl)-carbonyl group having optionally one or more halogen, hydroxy or C1-3 alkoxy substituents which may be the same or different, furthermore a pyridylcarbonyl, a pyrazinylcarbonyl, a furylcarbonyl, a chloroacetyl or a C1-4 alkoxycarbonyl group, or R1 and R2 may form, together with the adjacent nitrogen atoms, a pyrazole ring having optionally a C1-6 alkyl substituent in position 4, with the proviso that one of R1 and R2 is always different from hydrogen, R3 stands for hydrogen, mercapto group, a C1-4 alkylmercapto group, amino group, a C1-4 alkylamino group, a piperazino group having optionally an N-alkyl or 2-pyridyl substituent, a morpholino group or a piperidino group, and R4 stands for hydrogen, halogen, C1-4 alkyl or C1-4 alkoxy group. The compounds of the formulae (I) and (Ia) are prepared by acylating the respective 2,4,5-unsubstituted 4,5-dihydro-benzo-as-triazine derivatives. The new compounds of the formulae (I) and (Ia) possess analgesic, antiphlogistic and narcosis-potentiating effects.
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- Pharmaceutical composition and process of treatment
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A process for alleviating proliferative skin diseases such as psoriasis, atopic dermatitis, etc. comprising administering to humans, or domesticated animals, topically and/or systemically a composition comprising a pharmaceutical carrier and at least one active compound selected from the groups, substituted alkyl zanthines, tricyclic antidepressants, organic nitrates, antihypertensives, anti-asthma agents and central nervous system depressants and combinations of certain compounds from specifically named groups of compounds.
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