Item Code

Item name

Main contents

Objective and requirements

Key points and difficulties

Class

hour

Instruments

And amount

1

Synthesis of

Phenytoin Soidum

1. Benzoin condensation reaction (Preparation of Benzoin).

2. Oxidation reaction (Preparation of 1, 2-diphenylethane-1, 2-dione).

3. Benzilic acid rearrangement and condensation reaction (preparation of Phenytoin).

4. Preparation of phenytoin sodium.

1. Master the synthetic principle of phenytoin sodium

2. Learn the oxidation techniques with FeCl₃.

3. Study the mechanism of benzilic acid rearrangement.

1. The benzoin condensation reaction with vitamine B1 as a catalyst.

2. The mechanism of benzilic acid rearrangement.

9

Magnetic stirrer，water pump，whole set glass apparatus with standard joint.30sets

2

Synthesis of Procaine

Hydrochloride

1. Esterification (Preparation of Nitrocaine)

2. Reduction Reaction (Preparation of 2-(diethylamino)ethyl 4-aminobenzoate)

3. Preparation of Procaine hydrochloride and refinement

1. Master the synthetic principle of Procaine Hydrochloride.

2. Learn the experimental method of esterification and reduction.

3. Learn the principle and method of azeotropic distillation.

1. The esterification of an acid and an alcohol assisted with azeotropic distillation.

2. The reduction of nitro group with Fe/HCl.

9

Magnetic stirrer，water pump，whole set glass apparatus with standard joint.30sets

3

Synthesis of Sodium sulfacetaminde

1. Preparation of crude sodium sulfacetamide

2. Preparation of sulfacetamide

3. Peparation of sodium sulfacetamide

4. Discuss the designed experiment—method to synthesize dihydropyridine derivative.

1. Master the synthetic principle of sodium sulfacetaminde.

2. Master the skill of purification by changing pH.

3. Design the feasible method for dihydropyridine derivatives by literature searching.

1. The purification of product by changing pH and determine the main product at different pH.

9

Magnetic stirrer，water pump，whole set glass apparatus with standard joint.30sets

4

Synthesis of Dihydropyridine derivatives

1. Preparation of 3-nitrobenzaldehyde

2. Preparation of 2,6-dimethyl-3,5-diethoxycarbony-1,4-dihydropyridine.

1. Train the skill and ability of carrying out the drug synthesis independently.

2. Familiar with the process of medicinal chemistry in new drug research and quality control of the intermediate and the final product.

1. Master the skill of literature searching and experimental designing independently.

9

Magnetic stirrer，water pump，whole set glass apparatus with standard joint.30sets