Efficient synthetic routes to pyrazolo[3,4-b]indoles and pyrazolo[1,5-a]benzimidazoles via intram... more Efficient synthetic routes to pyrazolo[3,4-b]indoles and pyrazolo[1,5-a]benzimidazoles via intramolecular palladium- and copper-catalyzed cyclization of 1-aryl/1-unsubstituted 5-(2-bromoanilino)pyrazole precursors via intramolecular C-C and C-N bond formation have been reported.
A number of dibenzoxepine derivatives containing a fused heterocyclic ring at the 4,5-position ar... more A number of dibenzoxepine derivatives containing a fused heterocyclic ring at the 4,5-position are known to display a wide range of biological activity, and have proven to be lead compounds for psychoactive drugs for the treatment of anxiety disorder, depression, and in particular ...
A novel unexpected anionic domino process involving n-BuLi-induced rearrangement of 3,3-bis(methy... more A novel unexpected anionic domino process involving n-BuLi-induced rearrangement of 3,3-bis(methylthio) or 3-methylthio-3-aryl/heteroaryl/alkyl-o-bromoarylacrylonitriles to o-cyanoarylacetylenes in synthetically useful yields has been reported. The scope and generality of the reaction has been examined, and a possible mechanism has been proposed.
This report describes the preparation of a series of 17 novel racemic spirocyclic scaffolds that ... more This report describes the preparation of a series of 17 novel racemic spirocyclic scaffolds that are intended for the creation of compound libraries by parallel synthesis for biological screening. Each scaffold features two points of orthogonal diversification. The scaffolds are related to each other in four ways: (1) through stepwise changes in the size of the nitrogen-bearing ring; (2) through the oxidation state of the carbon-centered point of diversification; (3) through the relative stereochemical orientation of the two diversification sites in those members that are stereogenic; and (4) through the provision of both saturated and unsaturated versions of the furan ring in the scaffold series derived from 3-piperidone. The scaffolds provide incremental changes in the relative orientation of the diversity components that would be introduced onto them. The scaffolds feature high sp 3 carbon content which is essential for the three-dimensional exploration of chemical space. This characteristic is particularly evident in those members of this family that bear two stereocenters, i.e., the two series derived from 3-piperidone and 3-pyrrolidinone. In the series derived from 3-piperidone we were able to "split the difference" between the two diastereomers by preparation of their corresponding unsaturated version.
Efficient synthetic routes to pyrazolo[3,4-b]indoles and pyrazolo[1,5-a]benzimidazoles via intram... more Efficient synthetic routes to pyrazolo[3,4-b]indoles and pyrazolo[1,5-a]benzimidazoles via intramolecular palladium- and copper-catalyzed cyclization of 1-aryl/1-unsubstituted 5-(2-bromoanilino)pyrazole precursors via intramolecular C-C and C-N bond formation have been reported.
A number of dibenzoxepine derivatives containing a fused heterocyclic ring at the 4,5-position ar... more A number of dibenzoxepine derivatives containing a fused heterocyclic ring at the 4,5-position are known to display a wide range of biological activity, and have proven to be lead compounds for psychoactive drugs for the treatment of anxiety disorder, depression, and in particular ...
A novel unexpected anionic domino process involving n-BuLi-induced rearrangement of 3,3-bis(methy... more A novel unexpected anionic domino process involving n-BuLi-induced rearrangement of 3,3-bis(methylthio) or 3-methylthio-3-aryl/heteroaryl/alkyl-o-bromoarylacrylonitriles to o-cyanoarylacetylenes in synthetically useful yields has been reported. The scope and generality of the reaction has been examined, and a possible mechanism has been proposed.
This report describes the preparation of a series of 17 novel racemic spirocyclic scaffolds that ... more This report describes the preparation of a series of 17 novel racemic spirocyclic scaffolds that are intended for the creation of compound libraries by parallel synthesis for biological screening. Each scaffold features two points of orthogonal diversification. The scaffolds are related to each other in four ways: (1) through stepwise changes in the size of the nitrogen-bearing ring; (2) through the oxidation state of the carbon-centered point of diversification; (3) through the relative stereochemical orientation of the two diversification sites in those members that are stereogenic; and (4) through the provision of both saturated and unsaturated versions of the furan ring in the scaffold series derived from 3-piperidone. The scaffolds provide incremental changes in the relative orientation of the diversity components that would be introduced onto them. The scaffolds feature high sp 3 carbon content which is essential for the three-dimensional exploration of chemical space. This characteristic is particularly evident in those members of this family that bear two stereocenters, i.e., the two series derived from 3-piperidone and 3-pyrrolidinone. In the series derived from 3-piperidone we were able to "split the difference" between the two diastereomers by preparation of their corresponding unsaturated version.
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Papers by Sarvesh Kumar