- CNS-agent precursor: A simple and efficient synthesis of an antipsychotic drug fluanisone
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An efficient synthesis of antipsychotic drug fluanisone has been carried out in seven steps with an overall yield of 32.2%. The synthesis was started from 4-fluorobenzaldehyde. All the reactions were very clean and the isolation of products was very easy.
- Narsaiah, A. Venkat,Nagaiah,Devi, B. Karuna
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p. 829 - 832
(2012/11/07)
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- Process for the production of dry pharmaceutical forms and the thus obtained pharmaceutical compositions
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A process for the production of a solid dispersion of at least one therapeutic agent in a hydrophilic carrier having enhanced solubility in an aqueous media comprising dissolving at least one therapeutic agent in a volatile organic solvent containing a very hydrophilic polymer and evaporating the solvent to dryness; to form a co-precipitate of therapeutic agent and hydrophilic polymer. This invention relates to the resulting products and to their therapeutic method of use.
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- Process for the production of dry pharmaceutical forms and the thus obtained pharmaceutical compositions
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A process for the production of a solid dispersion of at least one therapeutic agent in a hydrophilic carrier having enhanced solubility in an aqueous media comprising dissolving at least one therapeutic agent in a volatile organic solvent containing a very hydrophilic polymer and evaporating the solvent to dryness to form a co-precipitate of therapeutic agent and hydrophilic polymer and the resulting products and their therapeutic method of use.
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- Piperazinobutyrophenone derivatives
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Central nervous system active butyrophenone derivatives in which γ -piperazinobutyrophenone derivatives of the formula, SPC1 Wherein R1 is hydrogen, amino, C1 -C5 alkanoylamino, C1 -C4 alkylamino or N-(C1 -C4 alkyl)(C1 -C5 alkanoyl) amino; R2 is hydrogen or halogen; R3 is hydrogen, halogen, C1 -C4 alkyl, C1 -C4 alkoxy or trifluoromethyl; and m is 0, 1 or 2, and acid addition salts thereof, can be prepared by reacting an indole derivative of the formula, SPC2 Wherein R2, R3 and m are the same as defined above, and R4 and R5 are hydrogen or C1 -C4 alkyl respectively, with an oxidizing agent to yield an o-alkanoylamino-γ-piperazinobutyrophenone derivative of the formula, SPC3 Wherein R2, R3, R4, R5 and m are the same as defined above, and further, if necessary, hydrolyzing the product to yield an o-amino-γ-piperazinobutyrophenone derivative of the formula, SPC4 Wherein R2, R3, R5 and m are the same as defined above, and further diazotizing, if desired, in case R5 is hydrogen, the obtained o-amino-γ-piperazinobutyrophenone derivative and subsequently decomposing the resultant diazonium compound to replace the diazonium group by hydrogen. Among the butyrophenone derivatives thus obtained, those in which R1 is amino, alkanoylamino, alkylamino or N-alkylalkanoylamino and those in which R1 is hydrogen and R2 is halogen substituted at meta-position to carbonyl group are novel compounds.
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