奈玛特韦:手性杂质分析和控制策略,推荐阅读原文

文摘   2024-11-18 07:03   天津  
nirmatrelvir的结构如下

Figure 2. Chromatograms of the achiral method (a) to separate 3 (spiked) from nirmatrelvir and (b) degradation of nirmatrelvir to 3 in a 0.1 M NaOH solution.


Figure 3. Isomeric control points for nirmatrelvir.


Origin of Diastereomeric Impurities Considered in the Nirmatrelvir Control Strategy from 4


Scheme 2. Origin of Diastereomeric Impurity Considered in the Nirmatrelvir Control Strategy from 5


Scheme 3. Origin of Diastereomeric Impurities Considered in the Nirmatrelvir Control Strategy from 6


Figure 4. Rationale on isomers considered to elucidate stereoisomer A.


Scheme 4. Synthetic Route to Potential Stereoisomer A


Figure 5. Achiral (a) and chiral (b) SFC methodology to determine absolute configuration of “stereoisomer A”.


Table 2. Nirmatrelvir Chiral Control Strategy Summary


Table 3. Chiral Control Strategy of Nirmatrelvir Starting Materials



https://doi.org/10.1021/acs.oprd.4c00392 
Building and Evolving a Chiral Control Strategy for Accelerated COVID Programs

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