Series 4 Synthesis Update - June 2018

[david1597]

We're at a busy time with synthesis in series 4. This is the collective work of many contributors. Those active in the lab include @edwintse, @maratsydney, @david1597, @Plebellec and @CamilleHauguel, along with @mattodd, @mcoster, @MedChemProf and @alintheopen with their students.

One thread is exploration of the RHS following a promising indole compound obtained from some Suzuki chemistry. This was followed up with many more analogues in April. A further set will be sent for testing next week.

On the LHS, the Pfizer compound continues to be a lead. A chemical synthesis of the original compound and a couple more of these 'OHOH' compounds have been made and will be sent for testing next week. A number of related 2-phenyl-propan-1-ol's are being actively explored, and related benzylic amine compounds are also now proposed.

Also currently active are ethers and amines in the 5-position. Ethers have already been successful. The amine work is still active.

Other new linkers on the pyrazine that do not yet exist in our library are also being investigated including carbamates and ureas.

A good number of compounds from the DCNYS have been successfully made recently: the HERG evador, the Nemesis and the phenylalaninol.

A further carborane compound has been made, following a highly potent one from last year.

Undergraduate classes have also been actively contributing. The Sydney 2018 SSP class have been working on a set of compounds and the Griffith GRIDD team are functionalising the 8 position.

And lastly, it's not just humans involved in the synthesis effort. Further biosynthesis is also underway at Pfizer.

[MFernflower]

Friendly reminder: This thread needs updating as many of these compounds have been completed and have been send out for testing as per #54

@david1597

Here's wishing good luck to all in the labs!!

[MFernflower]

Close as per #54