Publicação de Thomas Scattolin

Our recent work on one key starting material of adagrasib, the API used in KRAZATI, was just published in OPR&D. The cyclic amino β-ketoester was manufactured in a three-step telescoped process on >100 kg scale with an overall yield of 70%. Some important takeaways: ✔ By-product(s) of a transformation – waste for some, treasure to others: NaBr generated in the first step was critical to the success of the second alkylation. ✔ Counterion effect – often disregarded, usually impactful: LiHMDS and NaHMDS displayed completely different reactivity in the final Dieckmann condensation. ✔ Quench and crystallization – developing robust, reproducible and cleaner chemistry is really half the job, getting the pure compound out is often overlooked but as (if not more) critical. A great pleasure to have collaborated with an excellent team of professionals across multiple organizations. #OPRD #adagrasib #MRTX849 #ketoester https://lnkd.in/gC5ZNZyH

Happy to share that our process development work on the SOS1 inhibitor MRTX0902 was published in OPRD. Definitely a significant team effort, thanks to all involved! #miratiemployee #OPRD #oncology #MRTX0902 https://lnkd.in/gH4HK2wp

Great collaboration between PharmaBlock Group and Mirati Therapeutics CPR&D team. This work would not have been possible without the expertise of the excellent Mirati Drug Discovery team involved in this project [John Ketcham, Chris Smith FRSC, Matthew Marx]. MRTX0902 is a novel SOS1 inhibitor and was recently prepared in multi-kilogram scale to support clinical development studies. Link to the preprint on ChemXriv: https://lnkd.in/gGdPRYif Link to the J. Med. Chem. manuscript: https://lnkd.in/gEVihtAz #CPRD #miratiemployee #chemXriv #MRTX0902

Happy to share the first paper of the CPR&D team at Mirati Therapeutics. The described protocol showcases the removal of Cbz and Alloc protecting group under nucleophilic conditions mediated by 2-mercaptoethanol. This method is a great addition to the existing deprotection conditions as it expands the functional group tolerance for substrates bearing sensitive moieties to these more traditional approaches. #OrgLett

At Mirati Therapeutics, our team is comprised of passionate and collaborative individuals looking to make a positive impact on the lives of others. Sound like you? Find us at the #AACR21 Virtual Career Fair on May 17th. Register here https://bit.ly/3emadTE #Mirati_Employee

Our latest research from the Schoenebeck group (with Samir Bouayad-Gervais and Franziska Schoenebeck) on the general synthesis of N-trifluoromethylated carbonyl motifs was accepted in Nature! Various amides, (thio)carbamates and ureas could easily be accessed from the corresponding N-trifluoromethylcarbamoyl fluoride intermediates. Find out more https://lnkd.in/eabEFF7 #Nature