Process for producing dihydro-2H-pyran derivatives

摘要

Disclosed is a process for preparing dihydro-2H-pyran derivatives of formula I:;wherein R1 and R2 are defined herein. The process of the invention provides the compound of formula I in concise cascade reactions and in one pot. The compound of formulae I prepared by the process of the invention and its further transformed derivatives are useful for making pharmaceutical composition for the treatment of proliferative diseases.

主权项

1. A process for preparing dihydro-2H-pyran derivatives of formula I: wherein R1 is alkyl, cycloalkyl, aryl, heterocycloalkyl or heteroaryl, which is optionally substituted with one or more substituent selected from the group consisting of alkyl, alkenyl, alkynyl, alkoxy, nitro, cyano, halogen, hydroxyl, mono- or polyhalo alkyl, mono- or polyhalo alkoxy and phenyl; and R2 is alkyl or benzyl;which process comprises reacting aldehydes of the following formula:
R1—CHO wherein R1 is as defined in the above;with pyruvates of the following formula: wherein R2 is as defined in the above;in the presence of catalytic amount of β-proline.