Publications by authors named "Xin-Yu Da"
A biocatalytic approach for the synthesis of metaxalone and its analogues was developed based on the reaction of epoxides and cyanate catalyzed by halohydrin dehalogenase. Gram-scale synthesis of chiral and racemic metaxalone was achieved with 44% (98% ) and 81% yields, respectively, by protein engineering of the halohydrin dehalogenase HHDHamb from . Additionally, various metaxalone analogues were synthesized at 28-40% yields (90-99% ) for chiral forms and 77-92% yields for racemic forms.
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- Enantiopure β-nitroalcohols are vital for synthesizing pharmaceutical compounds, particularly β-adrenergic blockers.
- The study showcases the engineered enzyme HHDHamb, which allows for the selective bio-nitration of phenyl glycidyl ethers to produce chiral β-nitroalcohols using safe nitrite nitrating agents.
- The method achieved high yields and optical purity, and successfully synthesized two enantiomers of the β-adrenergic blocker metoprolol using these β-nitroalcohols as starting materials.