Strategy for the synthesis of pharmaceutical substances

elementary

P7S_WG CH2_W03 lists the differences between chemical and

pharmaceutical substances

P7S_WG CH2_W03 characterizes the advantages of convergent synthesis

compared to other synthetic strategies

P7S_WG CH2_W03 characterizes the properties of polymorphs and their

methods identification and indicates the selection criteria

of an appropriate polymorph for the active ingredient of

the drug

P7S_WG CH2_W03 explains the importance of selected methods of organic

synthesis in drug substance preparation

The aim of the lecture is to present the general principles of designing a synthesis strategy on the example of selected groups of pharmaceutical substances and to present the specific properties of pharmaceutical substances, methods of their synthesis, and structural analysis.

The aim of the lecture is to present the general principles of designing a synthesis strategy on the example of selected groups of pharmaceutical substances and to present the specific properties of pharmaceutical substances, methods of their synthesis and structural analysis.

Separate lectures will present in a multimedia form (PowePoint) detailed issues concerning the characteristics and properties of pharmaceutical substances, in comparison to chemical substances, synthesis strategies, with particular emphasis on strategies preferred in the synthesis of pharmaceutical substances. Basic issues related to the protection of intellectual property will be presented, including the basic principles and possibilities of patent protection. Sample description of national, European and US patents will be analyzed. Basic issues related to the diagnosis of polymorphism of pharmaceutical substances and its importance in obtaining the active substance of a medicinal product will be presented. Classical convergent synthesis of pharmaceutical substances from the taxane group, concurrent synthesis of pyrrolidinecarboxylic acids, linear synthesis of benzothiazoles and strategies for the synthesis of sulfonamides and triazines will be presented. Moreover, the possibilities of using pharmacophore groups of pharmaceutical substances in organic synthesis as groups activating the condensation processes of large structural fragments will be presented.

G. Patrick, Drug chemistry, short lectures, PWN 2009

A. Zejc, M. Gorczyca, Chemistry of drugs, PZWL 2008

Estimated student workload:

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task number of hours ECTS credits

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participation in classes 15 0.5

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preparation for classes 9

preparation for verification 32 1.5

consultation with the teacher 4

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1. Verification shows that:

- lists the differences between chemicals and pharmaceuticals without any noticeable shortcomings 5

- it calculates the differences between chemical substances and pharmaceutical substances almost fully, but it does not meet the criteria for a higher rating of 4.5

- to a large extent correctly calculates the differences between chemical substances and pharmaceutical substances, but does not meet the criteria for a higher rating 4

- to a large extent correctly but inconsistently characterizes the advantages of convergent synthesis compared to other synthesis strategies, but does not meet the criteria for a higher score 3.5

- in most test cases, it lists the differences between chemicals and pharmaceuticals, but does not meet the criteria for a higher grade 3

- does not calculate the differences between chemicals and pharmaceuticals, nor that it meets the criteria for a higher rating 2

2. Verification shows that:

- without noticeable shortcomings characterizes the advantages of converged synthesis compared to other synthesis strategies 5

- it almost fully correctly characterizes the advantages of converged synthesis compared to other synthesis strategies, but it does not meet the criteria for a higher rating of 4.5

- to a large extent correctly characterizes the advantages of converged synthesis compared to other synthesis strategies, but does not meet the criteria for a higher grade 4

- to a large extent correctly but inconsistently characterizes the advantages of convergent synthesis compared to other synthesis strategies, but does not meet the criteria for a higher score 3.5

- in most test cases, it lists the differences between chemicals and pharmaceuticals but does not meet the criteria for a higher rating 3

- does not demonstrate that it has the advantages of converged synthesis compared to other synthesis strategies, nor that it meets the criteria for a higher score 2

3. Verification does not show that:

- without noticeable shortcomings characterizes the properties of polymorphs and methods of their identification, and indicates the criteria for selecting the appropriate polymorph for the active substance of the drug 5

- it almost fully correctly characterizes the properties of polymorphs and the methods of their identification, and indicates the criteria for selecting the appropriate polymorph for the active substance of the drug, but does not meet the criteria for a higher rating of 4.5

- to a large extent correctly characterizes the properties of polymorphs and the methods of their identification, and indicates the criteria for selecting the appropriate polymorph for the active substance of the drug, but does not meet the criteria for a higher rating 4

- to a large extent correctly but inconsistently characterizes the properties of polymorphs and methods of their identification and indicates the criteria for selecting the appropriate polymorph for the active substance of the drug, but does not meet the criteria for a higher rating 3.5

- in most test cases, it characterizes the properties of polymorphs and methods of their identification, and indicates the criteria for selecting the appropriate polymorph for the active substance of the drug, but does not meet the criteria for a higher rating 3

- does not characterize the properties of polymorphs and the method of their identification and indicates the criteria for selecting the appropriate polymorph for the active substance of the drug, and that it meets the criteria for a higher score 2

4. Verification shows that:

- explains the importance of selected methods of organic synthesis in drug synthesis without noticeable shortcomings 5

- almost fully correctly explains the importance of selected methods of organic synthesis in the synthesis of drugs, but does not meet the criteria for a higher rating of 4.5

- to a large extent correctly characterizes the properties of polymorphs and the methods of their identification, and indicates the criteria for selecting the appropriate polymorph for the active substance of the drug, but does not meet the criteria for a higher rating 4

- largely correctly but inconsistently explains the importance of selected methods of organic synthesis in the synthesis of drugs, but does not meet the criteria for a higher rating 3.5

- in most test cases it explains the importance of selected methods of organic synthesis in drug synthesis but does not meet the criteria for a higher grade 3

- does not explain the importance of selected methods of organic synthesis in the synthesis of drugs, nor that it meets the criteria for a higher grade 2

The final grade x is derived from the value

st (w) = 5 if 4.5? w; st (w) = 4.5, if 4.25 <w ≤ 4.5; st (w) = 4 if 3.75 <w ≤ 4.25; st (w) = 3.5, if 3.25 <w ≤ 3.75; st (w) = 3 if 2.75 <w ≤ 3.25; st (w) = 2 if w ≤ 2.75

and based on the following rule:

● x is determined from the formula x = st (z), where z is the weighted average of the grades from the verifications carried out, where the exam grade weights are 2, and the grades weights for other forms of verification are 1

not relevant