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Medicinal Chemistry: Synthesis in Drug Discovery

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17 Questions

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

To synthesize a clinical candidate as efficiently and safely as possible

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

Modification of natural products

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

Higher overall yield

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

To disconnect the target compound into smaller fragments

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

To optimize lead compounds for PD and/or PK

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

To derivitize a lead compound into multiple analogs

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

To form the carbon-nitrogen bond

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

As a catalyst

What is the purpose of the mCPBA oxidation step?

To oxidize the sulfur atom

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

To protect the amine group

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

To brominate the alkyl chain

What is the overall goal of the synthesis route?

To develop an analog-friendly route

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

11 steps

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

0.8 nM

What is the final step in the preparation of analogs?

Analoging step

What is the condition used for the reflux reaction?

Reflux in MeOH

What is the advantage of the reported synthesis route?

It is a scaleable synthesis with little/no chromatography

Learn about the synthesis of drug analogs and clinical candidates in medicinal chemistry. Explore the process of hit identification, lead optimization, and development synthesis. Discover the importance of efficient and safe synthesis in drug discovery.

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