Tag filter: Green Chemistry

2022

Development of a Process to a 4-Arylated 2-Methylisoquinolin-1(2H)-one for the Treatment of Solid Tumors: Lessons in Ortho-Bromination, Selective Solubility, Pd Deactivation, and Form Control

Org. Process Res. Dev. 2022, 26, 5, 1458–1469

By: Antonio M. Ruda, Nadia Fleary-Roberts, Jonathan D. Moseley and Siân M. Forsyth et al.

2022

Application of the Polonovski Reaction: Scale-up of an Efficient and Environmentally Benign Opioid Demethylation

Org. Process Res. Dev. 2022

By: Antonio M. Ruda, Sofia Papadouli, Vargini Thangavadivale, and Jonathan D. Moseley et al.

January, 2021

Novel Bromination Process slashes PMI

CatSci was tasked with designing a new bromination method for a key reaction intermediate. Use of bromine rendered the previous process unsuitable for a larger campaign and would require expensive and time-consuming alterations to the plant.

January, 2021

Route Redesign to Eliminate Use of PhOCN

The route supplied by the client involved the use of phenyl cyanate for functionalising a heterocyclic intermediate with a nitrile group. Its ongoing use would require cyanide monitoring, a dedicated waste stream treatment step, and there were concerns over the sourcing of material of appropriate quality over the long term.

December, 2020

Development of a Late-Stage Buchwald Amination

CatSci was tasked with the development of a regioselective Buchwald-Hartwig amination for the final bond forming step of an API. The inherited conditions were not robust with respect to reaction conversion leading to stability concerns.

December, 2020

Designing a Robust Scalable Catalytic Process

The client's Phase 1 process was struggling to deliver API in low kg qualities. In particular, Intermediate B was of variable quality, and residual metals were known to negatively affect the onward chemistry