联合应用化学合成与生物合成手段，开展“化学酶法合成”研究，将二者的优势特点整合优化。通过酶法转化、化学催化手段实现药物合成中的关键化学键形成和手性中心构建，简化合成路线，提高合成效率，降低生产成本，并且减少反应产生的废弃物，降低污染，创建绿色精准的新型合成模式，为合成路线创新和新药开发提供理想的解决方案。 研究方向包括以下三方面：
1. 通过基因挖掘手段寻找新的酶催化剂，对酶进行改造优化，发展新型酶催化反应；
2. 结合酶催化和化学合成策略制备重要化学中间体，推向活性天然产物和药物分子的合成；
3. 新药发现。

1. Liu, Z.;# Zhai, W.;# Zeng, Z.; Meng, X.; Shi, Y.; Huang, J.; Su, P.; Yan X.; Yang L.-C.* “Concise construction of β-branched aromatic D-amino acids via transaminase-catalyzed dynamic kinetic resolution” Nat. Commun. 2026, 17, 3591. (IF=15.7)
2. Ni, Z.;# Zhuang, J.;# Gao, Y.;# Gao, G.; Liu, Z.; Su, P.; Cheng, G.-J.;* Yang, L.-C.* “Steric-Adaptive Biocatalysis: Imine Reductase-Mediated Dynamic Kinetic Resolution for Atroposelective Synthesis of Hindered Biaryl Amines” Adv. Sci. 2025, e10455. (IF=14.3)
3. Liu, Z.-X.;# Chen, X.;# Gao, X.; Zhang, S.; Xing, C.; Wang, R.; Hu, K.* Yang, L.-C.* “A Novel Type of PSMA-Targeting Ligands via β Branched Aromatic α Amino Acid Modification, Bearing Enhanced Tumor Targeting and Reduced Renal Toxicity” J. Med. Chem. 2025, 68, 19661-19672. (IF=6.8)
4. Li, F.;# Yang, L.-C.;# Zhang, J.; Chen, J. S.; Renata, H.* “Stereoselective Synthesis of β-Branched Aromatic α-Amino Acids via Biocatalytic Dynamic Kinetic Resolution,” Angew. Chem., Int. Ed. 2021, 60, 17680-17685. (IF=16.82)
5. Yang L.-C.;# Wang, Y.-N.;# Liu, R.; Luo, Y.; Ng, X. Q.; Yang, B.; Rong, Z.-Q.; Lan, Y.;* Shao, Z.;* Zhao, Y.* “Stereoselective Access to [5.5.0] and [4.4.1] Bicyclic Compounds through Pd-Catalysed Divergent Higher-Order Cycloadditions,” Nat. Chem. 2020, 12, 860-868. (IF=21.687, C100)
6. Yang, L.-C.;# Tan, Z. Y.; Rong, Z.-Q.; Liu, R.; Wang, Y.-N.; Zhao, Y.* “Pd-Titanium Relay Catalysis Enables Switch of Alkoxide-π-Allyl to Dienolate Reactivity for Spiro-Heterocycle Synthesis," Angew. Chem., Int. Ed. 2018, 57, 7860-7864. (IF=12.257, C100)
7. Wang, Y.-N.;# Yang L.-C.;# Rong, Z.-Q.; Liu, T.-L.; Liu, R.; Zhao, Y.* “Pd-Catalyzed Enantioselective [6+4] Cycloaddition of Vinyl Oxetanes with Azadienes to Access Ten-Membered Heterocycles,” Angew. Chem., Int. Ed. 2018, 57, 1596-1600. (IF=12.257, C100)
8. Rong, Z.-Q.;# Yang, L.-C.;# Liu, S.; Yu, Z.; Wang, Y.-N.; Tan, Z. Y.; Huang, R.-Z.; Lan, Y.;* Zhao, Y.* “Nine-membered Benzofuran-Fused Heterocycles: Enantioselective Synthesis by Pd-Catalysis and Rearrangement via Transannular Bond Formation” J. Am. Chem. Soc. 2017, 139, 15304-15307. (IF=14.357, C100)
9. Yang, L.-C.;# Rong, Z.-Q.;# Wang, Y.-N.; Tan, Z. Y.; Wang, M.; Zhao, Y.* “Construction of Nine-Membered Heterocycles through Palladium-Catalyzed Formal [5+4] Cycloaddition,” Angew. Chem., Int. Ed. 2017, 56, 2927-2931. (IF=12.102, C100)
10. Yang, L.-C.;# Wang, Y.-N.; Zhang, Y.;* Zhao, Y.* ACS Catal., 2017, 7, 93-97. “Acid-Assisted Ru-Catalyzed Enantioselective Amination of 1,2-Diols through Borrowing Hydrogen,” (IF=11.403)