Synthesis of Chiral Tetrahydrofuran Building Blocks from Pantolactones: Application in the Synthesis of Empagliflozin and Amprenavir Analogs,European Journal of Organic Chemistry

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Synthesis of Chiral Tetrahydrofuran Building Blocks from Pantolactones: Application in the Synthesis of Empagliflozin and Amprenavir Analogs
European Journal of Organic Chemistry ( IF 2.5 ) Pub Date : 2019-07-26 , DOI: 10.1002/ejoc.201900718
Paresh R. Athawale _{1,

2} , Neeta Kumari ₁ , Monica R. Dandawate ₁ , K. Kashinath _{1,

2} , D. Srinivasa Reddy _{1,

2}

Affiliation

Chiral 4,4–dimethyl tetrahydrofurans were synthesized using a chiral pool approach starting from both pantolactones. The synthesized building blocks are substituted with azide, amine, or alcohol groups making them interesting for applications in medicinal chemistry. Two of the synthesized building blocks were utilized for the synthesis of new analogs of amprenavir (protease inhibitor – anti HIV) and empagliflozin (SGLT2 inhibitor – anti‐diabetic).

中文翻译：

泛内酯合成手性四氢呋喃结构单元：在依帕格列净和安普那韦类似物的合成中的应用

从两个泛内酯开始，采用手性库法合成了手性4,4-二甲基四氢呋喃。合成的结构单元被叠氮化物，胺或醇基团取代，使其在药物化学中的应用很有趣。两个合成的构建基块用于合成氨普那韦（蛋白酶抑制剂–抗HIV）和依帕格列净（SGLT2抑制剂–抗糖尿病）的新类似物。

更新日期：2019-07-26

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