The total synthesis of sulfadiazine and silver sulfadiazine from readily available starting materials was adapted to semi-micro laboratory scale and is proposed as an experiment in drug synthesis for undergraduate courses.

Foram preparados complexos de inclusão de rifampicina (RP) com hidroxipropil-²-ciclodextrina (HP²CD). A solubilidade da RP em água aumentou linearmente com a concentração de ciclodextrina na faixa de concentração utilizada no diagrama de solubilidade. Os resultados foram analisados quantitativamente através do modelo de Higuchi e Connors. Os valores da constante de estabilidade (K) para o complexo RP/HP²CD em pH 6,9 foram 18 e 120-125 M-1 para as forças iônicas 0,01 e 0,18 M, respectivamente. A análise dos dados de deslocamento químico de ¹H e 15N-NMR para a RP livre e do complexo de inclusão RP/HP²CD revelou que somente os picos da cadeia lateral relacionada com o anel piperazina modificaram substancialmente, provavelmente devido à interação desta região da molécula da RP com a cavidade hidrofóbica da HP²CD. Com base no estudo de modelagem molecular foi proposta a estrutura otimizada para o complexo de inclusão RP/HP²CD. A estrutura proposta está de acordo com os resultados dos espectros de ¹H e 13C-NMR e 15N-NMR .

Inclusion complexes of rifampicin (RP) were prepared with hydroxypropyl-²-cyclodextrin (HP²CD). The aqueous solubility of RP increased linearly with cyclodextrin concentration in all range of the solubility diagram. The data was analyzed using the framework of Higuchi and Connors. The stability constant (K) values for RP/HP²CD complex at pH 6.9 were 18 and 120-125 M-1 for ionic strength 0.01 and 0.18M, respectively. The analysis of the chemical shift data of ¹H and 15N for free RP and RP/HP²CD inclusion complex reveal that only peaks of the side chain related to the piperazine ring of RP change substantially, probably due to interaction of this region of RP molecule with the hydrophobic core of HP²CD. We also postulated the optimized structure of RP/HP²CD inclusion complex using molecular modelling study. We found that the postulated structure was in agreement with ¹H and 13C-NMR and 15N-NMR spectra.

A simple laboratory technique is described for the synthesis of cyclopentadienylthallium and methylcyclopentadienylthallium and their use in the preparation of air sensitive metallocenes in solution. It does not use manifold, drybox or any other special glassware and was applied to the synthesis of cobaltocene, nickelocene and their methyl substituted analogs.