Cyclopropyl derivatives
A cyclopropyl group has been widely used to build SAR in medicinal chemistry. A cyclopropyl group is considered as an isostere of olefin (Bioorganic and Medicinal Chemistry Letter, 1996, 6(2), 213-218).
A cyclopropyl group could be used in SAR studies in place of a geminal-dimethyl group or a geminal-difluoro group.
A cyclopropyl group may provide metabolic stability because of its inherent bond angle.
However, the commercial availability of properly functionalized cyclopropyl derivatives is very limited. We have developed synthetic methods for a varieties of 1,1-disubstituted cyclopropyl derivatives anticipating their use in medicinal chemistry both in industry and academia. One substituent is an aryl group including heteroaryl, and other substituent is a polar functional group such as carboxylic acid, nitrile, amino, phenylcarbamate etc.
All these cyclopropyl derivatives are available in miligram to gram quantity. An order for a higher amount can be taken upon request.
The cyclopropyl moiety with carboxylic acid or amine could be used to construct amide bond. The cyclopropyl synthon with phenyl carbamate is a suitable precursor for isocyante for the synthesis of urea derivatives. Where as cyclopropyl derivatives with nitrile and imidamide could be used for the synthesis of complex heterocyclic ring or could be used in multicomponent reaction.
All our cyclopropyl synthons have low to medium molecular weights and contain only one reactive functional group and has no chiral center.
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phenyl)-cyclopropane-carboxylicacid.gif)
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phenyl)-cyclopropane-carbonitrile.gif)
phenyl)-cyclopropane-carbonitrile.gif)
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