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Lecturer:
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Teaching Division:
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Pharmaceutical Research Institute, Warsaw, Poland
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Educational and
professional goals:
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Learning of specific features of synthetic pharmaceutical substances; structural analysis and protection of intellectual properties. Gaining of the ability to design multi-step syntheses of selected classes pharmaceutical substances.
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Course description:
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Pharmaceutical substances - specific features as compared to other chemical compounds; certification and stability study. Polymorphism of pharmaceutical substances - generation and identification (XRPD, DSC, TGA; FT-IR, etc.); importance for finished product formulation. Strategies of multi-step pharmaceutical synthesis; advanced and key intermediates; Good Manufacturing Practice (GMP) concept. Linear, linear modified, convergent and concurrent strategies; principles of design of pharmaceutical synthesis. Use of patents for intellectual property protection; product patent and process patent; construction of a patent application. Convergent synthesis of prostanoids; coupling of alpha and omega side-chains with Corey lactone. Novel convergent synthesis of analogs of prostaglandin PGF2?. Convergent synthesis of taxanes; protection of cyclic skeleton (baccatin); linear and cyclic protections of side-chain; novel protection methods; conversion of paclitaxel into a docetaxel; synthesis of other antimitotic macrolides. Convergent synthesis of tetrazolylbiphenyl pharmaceuticals; Suzuki coupling - benefits and limits in scale-up of pharmaceutical syntheses. Linear synthesis of benzothiazoles and homochiral tetrahydrobenzothiazoles; regioselective functionalization of tetrahydrobenzothiazoles; benzothiazole activating group in organic synthesis. Concurrent synthesis of pyrrolidine carboxylic acids; classical and novel N-acylations (NEPA-NCA). Synthesis of triazines, diamino- and triamino-triazines; triazine super esters in organic synthesis.
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Required background:
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Principles of organic synthesis.
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Form of assessment:
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Written exam
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Remarks:
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Course on synthesis and basic analysis of selected classes of pharmaceutical substances.
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