Stereoselective process for preparing beta-anomer enriched 2-deoxy-2, 2-difluoro-d-ribofuranosyl-3, 5-hydroxy protected-1-alkyl and aryl sulfonate intermediates
申请人:ELI LILLY AND COMPANY
公开号:EP0640614A2
公开(公告)日:1995-03-01
A stereoselective process for preparing a β-anomer enriched 2-deoxy-2,2-difluoro-D-ribofuranosyl-3,5-hydroxy protected-1-alkyl and aryl sulfonate intermediates by contacting an α-anomer enriched 2-deoxy-2,2-difluoro-D-ribofuranosyl-3,5-hydroxy protected-1-fluoroalkyl and fluoroaryl sulfonate with a conjugate anion of a sulfonic acid containing the desired alkyl or aryl sulfonate.
一种制备富含 β-异构体的 2-脱氧-2,2-二氟-D-呋喃核糖基-3,5-羟基保护-1-烷基和芳基磺酸盐中间体的立体选择性工艺,其方法是将富含 α-异构体的 2-脱氧-2,2-二氟-D-呋喃核糖基-3,5-羟基保护-1-氟烷基和氟芳基磺酸盐与含有所需烷基或芳基磺酸盐的磺酸的共轭阴离子接触。