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SF5 building blocks: SF5-Blocks.
Jan 09 2012

New Products & Concept

SF5 building blocks: SF5-Blocks.

Dear Colleagues,

SpiroChem is happy to present a new range of products: the SF5-aromatics.

Until recently, the SF5 group was under-represented in drug discovery programs due to the scarcity of commercially available and synthetically useful products. We believe that this group has a promising future in life science research due to its interesting properties:

1) the volume of SF5 is larger than CF3 and slightly smaller than tert-butyl;[1]

2) the SF5 group is more electronegative than CF3;[2]

3) the SF5 group is very stable under strong acid and basic conditions.[3]

The utility of SF5 derivatives in drug discovery was recently showcased by Wipf and co-workers in the design of improved Mefloquine analogs.[4]

Therefore the SF5 group is a suitable tool to modulate the steric hindrance, lipophilicity and electronic properties of your candidates. It is also likely that this group will open new intellectual property space. This complements our library of building blocks for property modulation (oxetanes, azetidines, spirocycles, ...) and will soon become must-haves in the toolbox of discovery chemists in pharmaceutical and agrochemical companies.

SpiroChem has more than 60 derivatives in this new range of SF5-containing aromatics and, as usual, will keep adding new ones.[5] We also offer contract manufacturing services for specific derivatives so that you can focus your resources on what really matters: developing the drugs of tomorrow.

We wish you a happy and successful New Year 2012.


Your SpiroChem Team

[1] Lentz & Seppelt, In Chemistry of Hypervalent Compounds, K. Akiba, (Eds), Wiley-VCH, New York,1998, 295

[2] Sæthre, Berrah, Bozek, Børve, Carroll, Kukk, Gard, Winter & Thomas, J. Am. Chem. Soc. 2001, 123, 10729; Wipf, Henninger & Geib, J. Org. Chem. 1998, 63, 6088

[3] Bowden, Comina, Greenhall, Kariuki, Loveday & Philp Tetrahedron 2000, 56, 3399

[4] Wipf, Mo, Geib, Caridha, Dow, Gerena, Roncal & Milner Org. Biomol. Chem. 2009, 7, 4163

[5] Visit us at www.spirochem.com for information and prices

Some of our SF5-containing products: SF5-Blocks

And do not forget our other series of compounds! We keep adding new ones to our range of oxetane and azetidine-containing products. We also have kilograms of oxetan-3-one in stock (purity >98%) and the ability to produce more with excellent lead times.


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