Several 5-thio-substituted tetrazole derivatives were efficiently
synthesized by a three-step process. The substituted tetrazol-5-thiol,
namely, 1-benzyl-1H-tetrazol-5-thiol (2) was prepared by refluxing
commercially available benzyl isothiocyanate (1) with sodium azide in water.
The second step was the synthesis of 1-benzyl-5-[(3-bromopropyl)
thio]tetrazole (3) by thio alkylation of tetrazol-5-thiol (2) with 1,3-
dibromopropane in tetrahydrofuran. Finally, the 5-thio-substituted tetrazole
derivatives 4a-i were prepared by condensation of (3) with the corresponding
amine or thiol. The structures of the newly synthesized compounds were
characterized by NMR, LC/MS/MS, IR spectral data and elemental analysis. All
the synthesized compounds were screened for their antibacterial and
antifungal activities.
Studies of the degradation of olanzapine bulk drug under hydrolytic (acidic and alkaline), oxidising, and photolytic conditions are reported in this paper. Olanzapine is almost completely stable under photolytic and hydrolytic (acidic and alkaline) conditions. The major degradation products formed when olanzapine bulk drug was exposed to oxidative stress conditions were isolated by preparative reversed-phase highperformance liquid chromatography and characterized by FTIR, LC-MS-MS, and 1 H, 13 C, and DEPT NMR. On the basis of results from spectroscopy the degradation products were characterized as 10-hydroxy-2-methyl-5,10-dihydro-4H-benzoand 2-methyl-10-(2-methyl-10H-benzo[b]thieno[2,3-e][1,4] diazepin-4-yloxy)-5,10dihydro-4H-benzo[b]thieno[2,3-e]diazepin-4-one. Identification, isolation, and characterization of these oxidative degradation products are discussed in detail.
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