CAS: 1985605-59-1; (R)-12-((S)-7,8-Difluoro-6,11-Dihydrodibenzo[b,E]Thiepin-11-yl)-7-Hydroxy-3,4,12,12A-Tetrahydro-1H-[1,4]Oxazino[3,4-C]Pyrido[2,1-F][1,2,4]Triazine-6,8-Dione

上下游产品

3-(benzyloxy)-4-oxo-4H-pyran-2-carboxylate ethyl ester 1‐amino‐3‐(benzyloxy)‐4‐oxo-1,4-dihydropyridine‐2‐carboxylic acid ethyl ester 7-(benzyloxy)-3,4,12,12a-tetrahydro-1H-[1,4]oxazino[3,4-c]pyrido [2,1-f][1,2,4]triazine-6,8-diketone (R)-7-(benzyloxy)-3,4,12,12a-tetrahydro-1H-[1,4]pyrano[4,3-c]pyrido[2,1-f][1,2,4]triazine-6,8(1H,3H)-dione

3-(苄氧基)-4-氧代-4H-吡喃-2-羧酸置于吗啉,吡啶,盐酸,四(三苯基膦)钯,甲烷磺酸,Propanephosphonic Anhydride,4-甲基苯磺酸吡啶,四氯化锡,Potassium Carbonate,1,8-二氮杂双环[5.4.0]十一碳-7-烯,Lithium Chloride体系中,用 四氢呋喃,乙醇,N,N-二甲基乙酰胺,乙酸乙酯,N,N-二甲基甲酰胺,乙腈 用作溶剂,化学反应 65.5H,反应生成巴洛沙韦
参考文献:Baloxavir Marboxil 合成的第一代工艺开发:制备 Baloxavir Marboxil 中间体的合成方法的早期开发
标题:Baloxavir Marboxil 合成的第一代工艺开发:制备 Baloxavir Marboxil 中间体的合成方法的早期开发
摘要:本文描述的是制备手性三嗪酮 R-3 和非对映异构体中间体 5 的方法的发现和开发,这是合成帽依赖性核酸内切酶抑制剂 Baloxavir Marboxil (1) 的关键中间体,可抑制流感病毒的复制.手性三嗪酮 R-3 通过光学拆分其外消旋形式 Rac-3 获得.使用t3P和msoh的组合,通过三嗪酮r-3和硫杂苯醇4的缩合反应得到非对映体中间体5.这些反应在公斤级上成功进行,对于巴洛沙韦马波西生产工艺的建立至关重要.
Doi:10.1021/acs.Oprd.3C00514

专利信息

专利号:US-2024024497-A1
优先权日:2020-08-06
标 题:Methods for the synthesis of protein-drug conjugates
发明人：BORCHARDT ALLEN; HUGHES ROBERT MICHAEL
权利人:CIDARA THERAPEUTICS INC
摘要:The present invention relates to methods for the synthesis of conjugates useful for the treatment of viral infections, e.g., conjugates containing inhibitors of viral neuraminidase (e.g., zanamivir or an analog thereof) linked to an Fc domain monomer.

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).

专利号:US-2023364251-A1
优先权日:2020-08-06
标 题:Methods for the synthesis of protein-drug conjugates
发明人：BORCHARDT ALLEN; HUGHES ROBERT MICHAEL
权利人:CIDARA THERAPEUTICS INC
摘要:The present invention relates to intermediates and methods for synthesizing protein-drug conjugates that can be used for the treatment of diseases and related conditions.

专利号:TW-202220698-A
优先权日:2020-08-06
标题:Methods for the synthesis of protein-drug conjugates

专利号:WO-2022032188-A1
优先权日:2020-08-06
标 题 :Methods for the synthesis of protein-drug conjugates

专利号:EP-4192512-A1
优先权日:2020-08-06
标题 :Methods for the synthesis of protein-drug conjugates