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SpiroKit 2

sp2 to sp3 Switch

Aryl amines are prevalent motifs in high-throughput screening libraries but have proven to be particularly disruptive in late-stage drug development because of their propensity to generate reactive metabolites. Moreover, many sp2-rich lead molecules fail due to their poor pharmacokinetic properties.

Thanks to their similarity in size and shape, conformationally restricted systems and particularly cage like systems are unique classes of sp3 rigid linkers able to mimic benzene moieties.

SpiroKit 2: sp2 to sp3 Switch

Why SpiroKit 2?

At SpiroChem, we strongly believe that switching from sp2 systems to  conformationally restricted sp3 systems is a powerful alternative, giving rise to compounds with outstanding intrinsic properties. For this reason, we designed SpiroKit 2 to help you:

  • Anticipate toxicity related attrition
  • Increase sp3 fraction
  • Enhance solubility
  • Fine-tune the geometry of your molecule
  • Replace structural alerts by safe motifs
  • Modulate lipophilicity
  • Improve oral absorption
  • Optimize patent coverage
SpiroKit 2: sp2 to sp3 Switch

Offered subsets

SPIROKIT 2a: Bicyclo[1.1.1]pentan-1-amine Derivatives

A selection of 9 bicyclo[1.1.1]pentan-1-amine derivatives diversifically substituted in position 3 and considered as priviligiated surrogates of substituted anilines.

SPIROKIT 2a is the must-have toolbox to have in stock for all your medchem programs to quickly evaluate the impact of the BCP motif on:

  • Activity
  • Solubility
  • Lipophilicity
  • Metabolism
Catalog ID Compounds Amount (each) Price
SPK2a 9 100mg CHF 2.150 USD 2.299
250mg CHF 4.290 USD 4.559
500mg CHF 6.890 USD 7.319
1000mg CHF 10.750 USD 11.429

SPIROKIT 2b is a selection of 7 di-amino rigid
sp3 systems and the must-have toolbox to:

  • Evaluate the optimum distance and angle between the two amino handles
  • Anticipate metabolism issue
  • Increase sp3 fraction
  • Modulate lipophilicity
  • Enhance solubility
  • Optimize patent coverage
Catalog ID Compounds Amount (each) Price
SPK2b 7 100mg CHF 1.860 USD 1.979
250mg CHF 3.870 USD 4.119
500mg CHF 6.200 USD 6.599
1000mg CHF 8.990 USD 9.959

A selection of 8 bifunctionalized rigid sp3 systems with an amino group and an ester as exit vectors.

SPIROKIT 2c is the must-have toolbox to:

  • Evaluate the optimum distance and angle between
    the amino and the ester handles
  • Anticipate metabolism issue
  • Increase sp3 fraction
  • Modulate lipophilicity
  • Enhance solubility
  • Optimize patent coverage
Catalog ID Compounds Amount (each) Price
SPK2c 8 100mg CHF 1.940 USD 2.059
250mg CHF 3.890 USD 4.139
500mg CHF 6.230 USD 6.629
1000mg CHF 10.890 USD 11.589

A selection of 9 bifunctionalized rigid sp3 systems with an amino group and a hydroxy group as exit vectors.

SPIROKIT 2c is the must-have toolbox to:

  • Evaluate the optimum distance and angle between the amino and the hydroxy handles
  • Anticipate metabolism issue
  • Increase sp3 fraction
  • Modulate lipophilicity
  • Enhance solubility
  • Optimize patent coverage
Catalog ID Compounds Amount (each) Price
SPK2d 9 100mg CHF 1.180 USD 1.259
250mg CHF 2.400 USD 2.559
500mg CHF 4.100 USD 4.369
1000mg CHF 5.860 USD 6.239
SpiroKit 2: sp2 to sp3 Switch

More Information

To receive more information about the SpiroKits, please contact Laurence Jung, PhD: laurence.jung@spirochem.com

SpiroKits

Other SpiroKits

SpiroKit 1

pKa-Tuned
Amines

SpiroKit 3

α,α Disubstituted Amino Acids

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