Advanced Techniques in Synthetic Organic Chemistry

Course objectives

To demonstrate and acquaint the participants with a broad selection of important, useful and advanced or difficult synthetic methods.

General contents and topics

Lab-techniques in organic synthesis related to important and non-conventional reactions that are difficult to perform, e.g.:

• Handling of reactive and sensitive reagents (butyllithium, low boiling liquids, liquid ammonia, liquid sulfur dioxide, etc.)
• Handling of small quantities of material.
• Methods for addition of reagents under special or difficult conditions (septum, syringe, cannulla, plastic bag techniques, etc.)
• Methods for mixing and stirring under intricate conditions.
• Methods for temperature regulation (reactions at excessive temperatures, programmed temperature, etc.)
• Selection of reaction vessels and performance of reactions under intricate conditions (screw cap sealed reaction vessels, special reactors, reactions under pressure or under inert atmosphere, balloon technique, bobblers, etc.)
• Methods for transport and filtration under intricate conditions (siphon-technique, pressure filtration, filtration under inert atmosphere, Schlenk technique, hot filtration, etc.)
• Reaction under inert atmosphere.
• Simple methods for programming and automatisation of lab-processes.
• Methods for optimisation of lab-processes.
• Chromatographic methods for checking purity and purification (preparative tlc, rotating disc tlc, flash chromatography, preparative hplc, etc.)
• Distillation and recrystallisation of small quantities.
• Ball tube distillation.
• Suitable and safe set-ups.

The techniques will be applied by means of the unit operations used in organic synthesis and they will be illustrated by means of important reactions such as alkylation, substitution, addition, elimination, organometallic chemistry, transition metal chemistry, hydrogenation, use of protecting groups, stereoselective synthesis, etc. If possible, problems that have posed an obstacle to the participants' daily work will be selected.

General information

Lab-course suitable for PhD students from all institutions of higher education. The course is open to other qualified chemists, e.g. from industry (bench space permitting). The course is basically a laboratory course, but it includes 12 lectures on the above topics as well as demonstrations, discussions of current problems of common interest, exchange of knowledge and experience and solution of practical problems in the laboratory. Emphasis is put on the demonstration and testing of methods rather than the preparation of specific target molecules. Each participant will be confronted with problems which require application of lab-techniques for their solution. It will be possible for the participants to follow and discuss problems and solutions with the other participants. The aim is to give an impression of the usage and potential of a range of general synthetic methods.

Duration

7 to 18 January 2002.

Course weight

0.083 STÅ (STÅ = student full-time equivalent) = 4.98 ECTS (European Credit Transfer System).

Course director

Professor Mikael Begtrup, Department of Medicinal Chemistry at The Royal Danish School of Pharmacy.

Course fee

Total: DKK 13,800 (including lunch),
of which operating costs amount to: DKK 2,800.
An additional amount for study materials: DKK 300.

Closing date for application

1 November 2001.

Course capacity

16 participants.

N.B.

Teachers: Experienced experimentalists from The Royal Danish School of Pharmacy, Carlsberg Laboratorium, The Technical University of Denmark, and The University of Copenhagen.

Study materials: M. Casey et al, "Advanced Practical Organic Chemistry", Blackie, London 1994 or equivalents is recommended.

Evaluation: No formal examination, but participants should have been present and demonstrated a satisfactory level of activity during 90 per cent of the course.