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- Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective . . .
The Supporting Information is available free of charge on the ACS Publications website at DOI: 10 1021 acs jmedchem 9b00687 Biochemical and cellular assay data for I-2 and I-3; evaluation of the BTK occupancy capability of studied compounds in mouse; fast dilution and protein precipitation experiment for 13 16 31a; serine mutant assay for 13 and 16; biochemical data for 20-int and 21-int; In
- The synthesis review of the approved tyrosine kinase inhibitors for . . .
Optimized synthesis route of Zanubrutinib In 2019, the optimized synthesis route has been reported in a Chinese patent by Xu et al [122] Starting from the coupling reaction between intermediate 290 and 296 , Zanubrutinib was prepared by five steps, including catalytic hydrogenation, Boc removal, and acylation, with overall yield of 51 4%
- WO2024110862A1 - Process for preparing zanubrutinib - Google Patents
The Zanubrutinib synthesis process is also described in WO 2018 033135 (WO'135) This process involves, among other steps, synthesis and isolation of an intermediate compound of formula (II) : formula II from an intermediate compound of formula (I) : formula I where X is Cl In this regard, see Step 13 on p 36 of WO'135, where the compound of
- How to synthesize Zanubrutinib? - ChemicalBook
Zanubrutinib is a drug that was shown to effectively treat cancer of B cells without causing severe excessive side effects ChemicalBook >> Articles Category List >> Inhibitors Synthesis method The most likely process synthesis, depicted below, began with benzoic acid 329 Reaction with malononitrile in refluxing ethyl acetate generated
- Synthesis of zanubrutinib (92) | Download Scientific Diagram - ResearchGate
Download scientific diagram | Synthesis of zanubrutinib (92) from publication: Tailor-made amino acid-derived pharmaceuticals approved by the FDA in 2019 | Amino acids (AAs) are among a handful of
- Asymmetric Synthesis of US-FDA Approved Drugs over Five Years . . . - MDPI
Asymmetric synthesis involves the conversion of an achiral starting material into a chiral product This review emphasizes the methods used for synthesizing FDA-approved chiral drugs during 2016–2020, with a special focus on asymmetric synthesis by means of chiral induction, resolution, or chiral pool Synthesis of Zanubrutinib Scheme 19
- Data-driven automatic synthesis planning: Synthesis routes of S . . .
1 Data-driven automatic synthesis planning: Synthesis routes of S-Zanubrutinib identified with CDI CASP Zhen Guo,1,2,4,* Akihiro Takada3 and Alexei A Lapkin1,2,4,* 1Chemical Data Intelligence (CDI) Pte Ltd, 9 Raffles Place #26-01, Republic Plaza Singapore, Singapore 048619 2Innovation Centre in Digital Molecular Technologies, Yusuf Hamied Department of Chemistry, University
- Zanubrutinib - an overview | ScienceDirect Topics
Zanubrutinib, a highly potent, selective, irreversible BTK inhibitor, was designed to maximize target occupancy and minimize off-target binding [119,120] The original synthesis route of Zanubrutinib reported in 2016 by Wang et al It began with the chlorination of 4-phenoxybenzoic acid (2 8 6), followed by carbonyl addition, etherification, cyclization, reduction, oxidation to get the
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