Development of an efficient and practical route for the multikilogram manufacture of the SRC kinase inhibitor AZD0530

Organic Process Research and Development

Volumn 14, Issue 5, 2010, Pages 1088-1093

  Ford, J Gair ^a   OKearney Mcmullan, Anne ^c   Pointon, Simon M ^c   Powell, Lyn ^c   Siedlecki, Paul S ^c   Purdie, Mark ^c   Withnall, Jane ^c   Frances Wood, Phil OKeefe ^b  

^a ASTRAZENECA   (United Kingdom)

^b Jealotts Hill International Research Station   (United Kingdom)

^c NONE

Author keywords

[No Author keywords available]

Indexed keywords

RESEARCH AND DEVELOPMENT; SRC-KINASE;

ENZYMES; INDUSTRIAL RESEARCH;

MANUFACTURE;

EID: 77956911021     PISSN: 10836160     EISSN: 1520586X     Source Type: Journal    
DOI: 10.1021/op100163m     Document Type: Article

References (5)

1. Hennequin, L. F.; Allen, J.; Breed, J.; Curwen, J.; Fennell, M.; Green, T. P.; Lambert van der Brempt C.; Morgentin, R.; Norman, R. A.; Olivier, A.; Otterbein, L.; Ple, P. A.; Warin, N.; Costello, G. J. Med. Chem. 2006, 49, 6465-6488
2. Ford, J. G.; Pointon, S. M.; Powell, L.; Siedlecki, P. S.; Baum, J.; Chubb, R.; Fieldhouse, R.; Muxworthy, J.; Nivlet, A.; Stenson, R.; Warwick, E. Org. Process Res. Dev. 2010, 14, DOI: 10.1021/op100161y.
3. Ford, J. G.; McCabe, J. F.; OKearney-McMullan, A.; OKeefe, P.; Pointon, S. M.; Powell, L.; Purdie, M.; Withnall, J. WO/2006/064217, 2006.
4. Yang, C.; He, G.; He, Y.; Ma, P. J. Chem. Eng. Data 2008, 53, 1639-1642
5. No allowances have been made for economies of scale; thus, the real reduction in costs will have been less than this. The new route produced >80 kg of AZD0530 difumarate, whereas the old route was used to produce 4.5 kg.