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US 9,630,940 B2Granted
Process for producing dihydro-2H-pyran derivatives
AssigneeOkinawa Institute of Science and Technology School Corporation
InventorsPandurang V. Chouthaiwale, Fujie Tanaka
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Abstract
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.
Claims6
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.
9 more elements
Dependencies are inferred from the claim text.