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Identify the reagents 5: answers

Back in August I posted a scheme for the synthesis of a late-stage intermediate towards PF-06826647, a compound identified by Pfizer as a potent and selective tyrosine kinase 2 (TYK-2) inhibitor. I asked if you could identify reagents or intermediates A, B and D. Below are the answers! You can read more here in the full

Identify the reagents 5: August 2021

The scheme below shows the synthesis of a late-stage intermediate towards PF-06826647, a compound identified by Pfizer as a potent and selective tyrosine kinase 2 (TYK-2) inhibitor that has entered phase 2 clinical trials for the treatment of autoimmune diseases. Can you identify intermediates A, B and D? Answers and a reference will be posted

Identify the reagents 4: answers

Last month I posted a scheme for the synthesis of a late-stage intermediate towards AZD9833, a compound identified by AstraZeneca as a selective estrogen receptor degrader (SERD) and antagonist that is currently in phase 2b clinical trials for the treatment of ER+ breast cancer. I asked if you could identify reagents or intermediates A-C. Below are

Identify the reagents 4: July 2021

The scheme below shows the synthesis of a late-stage intermediate towards AZD9833, a compound identified by AstraZeneca as a selective estrogen receptor degrader (SERD) and antagonist that is currently in phase 2b clinical trials for the treatment of ER+ breast cancer. Can you identify reagents or intermediates A, B and C? Answers and a reference

Identify the reagents 2- April 2021

A recent paper by a team from Merck describe the synthesis of a soluble guanylate cyclase (cGC) stimulator of interest for the treatment of hypertension. Can you identify reagents or intermediates B, F and the target compound H? Answers and a reference will be posted in May, along with another problem. Enjoy!

Identify the reagents 1: answers

Last month I posted a scheme from a paper by Jonathan H. George et al at the University of Adelaide describing a biomimetic total synthesis of the Rhododendron meroterpenoids rubiginosins A and G and asked if you could identify reagents or intermediates B, D, E and H. Below are the answers! You can read more here

Cyanomethylene trimethylphosphorane (CMMP)- a safer reagent for Mitsunobu couplings

The Mitsunobu reaction is a powerful coupling method for alkylation of various nucleophiles (H-A) with alcohols (R-OH).[1] The classical conditions use a redox system comprising of an azodicarboxylate (such as diethylaziodicarboxylate, DEAD) and a phosphine (normally triphenylphosphine, TPP). The alcohol is essentially activated in situ and coupling occurs with the generation of the phosphine oxide

Oiling the cogs- Practical tips, useful facts and resources: Organometallic highlight:

The generation of lithium-alkoxide based aryl and heteroaryl Grignard reagents by Mg-Br/Cl exchange in toluene- increased reactivity and wide applicability. Organomagnesium-based organometallics are used extensively in organic chemistry.[1] Historically the reagents were prepared by direct insertion of magnesium metal into organic halides. With demand for more industrially applicable methods, halogen-magnesium exchange using alkyl magnesium halides

Reagent of the month: Lithium Aluminium hydride

One might think that this hard-hitting, students best friend (it will reduce just about anything given the right conditions and is the go-to reducing agent for exam questions involving a reduction) has little more to offer to the practising chemist. However, a recent paper by Harder etal (Angew Chem Int Ed. 2018, 57(24), 7156) demonstrates

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