Lecture 5 - Stereochemistry of Drugs

Question 1

Eutomer

Answer 1

More potent enatiomer

Question 2

Distomer

Answer 2

Less potent enatiomer

Question 3

Problems with distomers

Answer 3

No activity, Less potent than eutomer adverse effects, different therapeutic effect

Question 4

How do companies avoid potential pitfalls in approval process due to problems of other stereoismers?

Answer 4

1. Pure starting material (Sugars, AA, Natural products)
2. Carboxylic acid or amine, can separate enantiomers at end by making diastereomeric salts
3. Enzymes
4. Use synthetic chiral catalyst
5. chromatography