A novel process for the preparation of [(R,S)/ (S,R)] and [(S,S)/ (R,R)] chroman epoxides, key intermediates in the synthesis of Nebivolol

Ravikanth Vysyaraju; Hanumantha Rao B.; Subramanyeswara Rao I.V.; Venkateswarlu J.; Prasada Rao K.V.V.; Siddaiah V.

doi:10.21746/ijbio.2017.06.007

A novel process for the preparation of [(R,S)/ (S,R)] and [(S,S)/ (R,R)] chroman epoxides, key intermediates in the synthesis of Nebivolol

Author(s): Ravikanth Vysyaraju, Hanumantha Rao B., Subramanyeswara Rao I.V., Venkateswarlu J., Prasada Rao K.V.V., Siddaiah V.*

Abstract

A novel, cost effective, scalable process for the preparation of chroman epoxides starting from 4-fluorophenol is described. The highlights of the process are single step O-acylation, fries rearrangement, one pot synthesis of claisen condensation, cyclization, reduction, epoxidation with over all yield of 50.9% [(R,S)/(S,R)]-chroman epoxide-A is 33.9% and [(S,S)/(R,R)]-chroman epoxide-B is 17%.

10.21746/ijbio.2017.06.007

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