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Medicinal Chemistry: Synthesis in Drug Discovery

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Medicinal Chemistry: Synthesis in Drug Discovery

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Questions and Answers

What is the primary goal of development synthesis in medicinal chemistry?

To synthesize a clinical candidate as efficiently and safely as possible (correct)

To optimize lead compounds for PD and/or PK

To synthesize multiple analogs efficiently

To identify the pharmacophore of a lead compound

Which approach to designing a synthetic route involves modifying natural products with a common structural motif?

Identification of compounds with similar structures

Retrosynthetic analysis

Modification of natural products (correct)

Linear synthesis

What is the primary benefit of convergent synthesis compared to linear synthesis?

Fewer reactions are required

Easier purification of products

More stereospecific reactions

Higher overall yield (correct)

What is the purpose of retrosynthetic analysis in designing a synthetic route?

To disconnect the target compound into smaller fragments Signup and view all the answers

What is the goal of hit to lead optimization in medicinal chemistry?

To optimize lead compounds for PD and/or PK Signup and view all the answers

What is the purpose of partial or semi-synthesis in medicinal chemistry?

To derivitize a lead compound into multiple analogs Signup and view all the answers

What is the purpose of the Suzuki Reaction in Step 3 of 10?

To form the carbon-nitrogen bond Signup and view all the answers

What is the role of Pd(PPh3)4 in the Suzuki Reaction?

As a catalyst Signup and view all the answers

What is the purpose of the mCPBA oxidation step?

To oxidize the sulfur atom Signup and view all the answers

What is the purpose of the Boc2O reaction in the first chromatography step?

To protect the amine group Signup and view all the answers

What is the purpose of the CuBr2 reaction in the final step?

To brominate the alkyl chain Signup and view all the answers

What is the overall goal of the synthesis route?

To develop an analog-friendly route Signup and view all the answers

What is the number of steps in the reported synthesis of chloropyridine advanced intermediate?

11 steps Signup and view all the answers

What is the IC50 value of PF-3514411 against CDK-2?

0.8 nM Signup and view all the answers

What is the final step in the preparation of analogs?

Analoging step Signup and view all the answers

What is the condition used for the reflux reaction?

Reflux in MeOH Signup and view all the answers

What is the advantage of the reported synthesis route?

It is a scaleable synthesis with little/no chromatography Signup and view all the answers