A Continuous Flow Chemistry Platform for Low Temperature Reactions

A low temperature reactor platform that facilitates metalation followed by electrophilic quenching, and related reactions under continuous flow-through conditions has been developed.

Pre-cooling loops are incorporated for all 3 reactor input streams and gaseous reagent inputs can be easily introduced by attaching a ‘tube-in’tube’ presaturation module.

All of the coil reactors and flow chemistry equipment described are are available from Uniqsis Ltd

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ENZALUTAMIDE

New Drug Approvals

Enzalutamide, MDV-3100
MDV3100 is an orally bioavailable, organic, non-steroidal small molecule targeting the androgen receptor (AR) with potential antineoplastic activity. MDV3100 (Enzalutamide) blocks androgens from binding to the androgen receptor and prevents nuclear translocation and co-activator recruitment of the ligand-receptor complex. It also induces tumour cell apoptosis, and has no agonist activity. Early preclinical studies also suggest that MDV3100 inhibits breast cancer cell growth.
1H NMR FROM THE NET

1H NMR PREDICT AND 13 C NMR PREDICT BELOW

COSY PREDICT

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PATENT
http://www.google.com/patents/WO2015063720A1?cl=en

Enzalutamide is chemically described as 4-{3-[4-cyano-3-(trifluoromethyl)phenyl] -5 ,5 -dimethyl-4-oxo-2-sulfanylideneimidazolidin- 1 -yl } -2-fluoro-N-methylbenzamide of Formula I.
FORMULA I
Processes for the preparation of enzalutamide are described in U.S. Publication Nos. 2007/0004753 and 2007/0254933 and PCT Publication Nos. WO 2007/127010, WO 2006/124118, and WO 2011/106570.
PCT Publication No. WO 2011/106570 discloses that the processes described in U.S. Publication Nos. 2007/0004753 and 2007/0254933 result in a 25% yield of…

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