CAS: 1985607-83-7; 7,8-Difluoro-6,11-Dihydrodibenzo[b,E]Thiepin-11-Ol

6-Cyano-2,3-Difluorobenzyl Bromide置于sodium Tetrahydroborate,四磷十氧化物,三乙胺体系中,用 5,5-Dimethyl-1,3-Cyclohexadiene,乙醇,水,丙酮 用作溶剂,化学反应 5.0H,反应生成7,8-二氟-6,11-二氢二苯并[b,E]噻吩-11-醇
参考文献:开发质量可控和可扩展的制备7,8-二氟-6,11-二氢二苯并[ B,E ]噻吩-11-Ol的方法:Baloxavir Marboxil的关键中间体
标题:开发质量可控和可扩展的制备7,8-二氟-6,11-二氢二苯并[ B,E ]噻吩-11-Ol的方法:Baloxavir Marboxil的关键中间体
摘要:描述了新颖的六步合成7,8-二氟-6,11-二氢二苯并[ B,E ]噻吩-11-Ol(1).从3,4-二氟-2-甲基苯甲酸开始,并使用二苯二硫作为理想的硫源,可以有效解决诸如苛刻的反应条件,使用有气味的苯酚等问题,这些问题可能会限制中试工厂的已知工艺.该新路线的大规模适用性已在公斤级生产中成功证明,可提供纯度为98.04%,总收率为75%的1.同时,对相应的杂质分布进行了详细研究并充分记录在案.
Doi:10.1021/acs.Oprd.9B00389

专利信息

专利号:WO-2023286078-A1
优先权日:2021-07-13
标题:An improved process for the preparation of an intermediate of baloxavir morboxil
发明人：TALASANI SHYAM SUNDER REDDY; BUDIDETI SHANKAR REDDY; KOTTE RAJASHEKAR; SATTI VENKATA REDDY; MALA NAGENDRA; MUDDASANI PULLA REDDY; NANNAPANENI VENKAIAH CHOWDARY
权利人:NATCO PHARMA LTD
摘要:The present invention provides an improved process for the preparation of (12aR)-3,4,12,12a-tetrahydro-7-(phenylmethoxy)-1H-[1,4]oxazino[3,4-c] pyrido[2,1-f] [1,2,4]triazine-6,8-dione of Formula (I). Formula I which is a key intermediate in the synthesis of Baloxavir Morboxil of Formula (II).