CAS: 981-34-0; Betamethasone 9,11-Epoxide

相似化合物

24916-90-3 14622-47-0 2884-51-7

上下游产品

CAS号56665-79-3 17-hydroxy-16be...

在 Sodium Hydroxide体系中,用 甲醇,二氯甲烷,水 作为反应溶剂,化学反应 3.0H,反应生成 倍他米松环氧水解物
参考文献:Process Improvements In The Synthesis Of Corticosteroid 9,11β-Epoxides
标题:Process Improvements In The Synthesis Of Corticosteroid 9,11β-Epoxides
摘要:Corticosteroid 9,11 Beta-Epoxides Are Key Intermediates In The Preparation Of Pharmaceutically Important Compounds Such As Betamethasone,Mometasone,Beclomethasone,And Dexamethasone. A New Process For The 9,11 Beta-Epoxide Was Developed Using A Pcl5-Mediated Regioselective Dehydration Of Ii Alpha-Hydroxysteroid To Form The Corresponding Delta (9,11) Double Bond. The Olefin Is Then Converted Into 9 Alpha,11 Beta-Bromoformate By Treatment With 1,3-Dibromo-5,5-Dimethyl Hydantoin (Dbh) In Dmf And Subsequently Cyclized To Produce The Desired 9,11 Beta-Epoxide Upon Treatment With Naoh. Major Process-Related Impurities Such As 21-Oh-Delta (9,11)-Triene,21-Oh-Delta (11,12)-Triene,21-Cl-Delta (9,11)-Triene,And Beta-Epoxide-21-Cathylate As Well As 11 Beta-Cl Are All Eliminated Or Minimized. This New Process Has Been Implemented In Our Manufacturing Facility In Full-Scale Production And Proved To Raise The Overall Yield And The Quality Of The Product Dramatically Compared To The Existing Process.
DOI:10.1021/op0102013