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Fast and Efficient Synthesis of Racemic Baloxavir Catalyzed by Strong Solid Acid under Microwave Conditions.
- Source :
- Crystals (2073-4352); Jul2022, Vol. 12 Issue 7, pN.PAG-N.PAG, 9p
- Publication Year :
- 2022
-
Abstract
- The compound (±)-12aR-12-[(11S)-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 is the intermediate of baloxavir marboxil. In the literature, traditional heating methods and common acid catalysts are used, which result in long reaction times and a low yield. Therefore, finding an efficient and environmentally friendly synthetic route is necessary. In this study, (±)-12aR-12-[(11S)-7,8-difluoro-6,11-dihydrodibenzo[b,e]thiepin-11-yl]-7-benzyloxy-3,4,12,12a-tetrahydro-1h-[1,4]oxazino[3,4-c]pyrido[2,1-f][1,2,4]triazine-6,8-dione (compound 3) was synthesized using a sulfonate resin solid acid catalyst (HND-580) under microwave conditions. The benzyl group was removed without further purification, and an intermediate, racemic baloxavir, was obtained under microwave irradiation. The total yield of the two steps was 78%. This method greatly reduces the reaction time and improves production efficiency. [ABSTRACT FROM AUTHOR]
- Subjects :
- MICROWAVES
ACID catalysts
BENZYL group
SOLIDS
ACIDS
Subjects
Details
- Language :
- English
- ISSN :
- 20734352
- Volume :
- 12
- Issue :
- 7
- Database :
- Complementary Index
- Journal :
- Crystals (2073-4352)
- Publication Type :
- Academic Journal
- Accession number :
- 158210920
- Full Text :
- https://doi.org/10.3390/cryst12070891