Synthesis method for preparing SGLT inhibitor intermediate

PH12023550668B1Active Publication Date: 2026-10-02DAEWOONG PHARM CO LTD
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Patent Information

Application Number
PH12023550668
Authority / Receiving Office
PH · PH
Patent Type
Patents
Current Assignee / Owner
Filing Date
2023-03-09
Publication Date
2026-10-02
Estimated Expiration
2043-03-09
Patent Text Reader

Abstract

A method for preparing compound 1 and compound 2 having a structure as shown below, the method comprises the following steps: Step 1-1) subjecting 2,3-dihydrobenzofuran-7-amine as a raw material to a selective dibromination with a brominating reagent to obtain 4,6-dibromo-2,3dihydrobenzofuran-7-amine; Step 1-2) subjecting 4,6-dibromo-2,3-dihydrobenzofuran-7-amine obtained in the step 1-1) to Sandmeyer reaction for chlorination to obtain 4,6-dibromo -7-chloro-2,3dihydrobenzofuran; Step 1-3) selectively debrominating from 4,6-dibromo-7-chloro-2,3dihydrobenzofuran obtained in the step 1-2) using a strong base, and then adding a formylation reagent to obtain compound 1; Step 2-1) selectively debrominating from 4,6-dibromo-7-chloro-2,3dihydrobenzofuran obtained in the step 1-2) using a strong base, and then reacting with 4-cyclopropyl benzaldehyde to obtain compound 2.
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