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?

<p>To disconnect the target compound into smaller fragments (C)</p> Signup and view all the answers

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

<p>To optimize lead compounds for PD and/or PK (A)</p> Signup and view all the answers

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

<p>To derivitize a lead compound into multiple analogs (C)</p> Signup and view all the answers

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

<p>To form the carbon-nitrogen bond (C)</p> Signup and view all the answers

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

<p>As a catalyst (D)</p> Signup and view all the answers

What is the purpose of the mCPBA oxidation step?

<p>To oxidize the sulfur atom (D)</p> Signup and view all the answers

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

<p>To protect the amine group (D)</p> Signup and view all the answers

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

<p>To brominate the alkyl chain (D)</p> Signup and view all the answers

What is the overall goal of the synthesis route?

<p>To develop an analog-friendly route (B)</p> Signup and view all the answers

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

<p>11 steps (D)</p> Signup and view all the answers

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

<p>0.8 nM (A)</p> Signup and view all the answers

What is the final step in the preparation of analogs?

<p>Analoging step (C)</p> Signup and view all the answers

What is the condition used for the reflux reaction?

<p>Reflux in MeOH (B)</p> Signup and view all the answers

What is the advantage of the reported synthesis route?

<p>It is a scaleable synthesis with little/no chromatography (D)</p> Signup and view all the answers

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