2024
DOI: 10.1021/acs.oprd.4c00049
|View full text |Cite
|
Sign up to set email alerts
|

Commercial Route Development Toward PF-07265807, an AXL-MER Inhibitor Oncology Candidate

Douglas J. Critcher,
Christopher Paul Ashcroft,
Alan J. Pettman
et al.

Abstract: Our route scouting efforts toward finding the most efficient construction of PF-07265807 (ARRY-067) in readiness for process development prior to commercial manufacture are described. ARRY-067 contains the azaindazole (1H-pyrazolo [3,4-b]pyridine) building block that is common to many pharmaceuticals and bioactive agents. Herein, our novel approach to this challenging structural motif is described where an oxazoline ring-opening cyclization cascade triggered by the addition of hydrazine reveals the target 3-al… Show more

Help me understand this report

Search citation statements

Order By: Relevance

Paper Sections

Select...
2

Citation Types

0
2
0

Year Published

2024
2024
2024
2024

Publication Types

Select...
2

Relationship

1
1

Authors

Journals

citations
Cited by 2 publications
(2 citation statements)
references
References 29 publications
0
2
0
Order By: Relevance
“…Disappointingly, the development of PF-07265807 by Pfizer has been discontinued; however, route scouting efforts to establish a suitable route for commercial manufacture were completed in a complementary manuscript recently published, and efforts toward assessing and developing a continuous flow process based on this route are described herein.…”
Section: Introductionmentioning
confidence: 99%
See 1 more Smart Citation
“…Disappointingly, the development of PF-07265807 by Pfizer has been discontinued; however, route scouting efforts to establish a suitable route for commercial manufacture were completed in a complementary manuscript recently published, and efforts toward assessing and developing a continuous flow process based on this route are described herein.…”
Section: Introductionmentioning
confidence: 99%
“…Additionally, flow offered the potential for using diluted solutions of hydrazine hydrate. The batch process used concentrated aqueous hydrazine solutions of 51–65 wt % hydrazine (80–100 wt % aqueous hydrazine) and operated at ambient conditions (25 °C) with a reaction time of ∼48 h to full conversion . Reducing the hydrazine concentration used in batch would drastically increase the reaction time further.…”
Section: Introductionmentioning
confidence: 99%