Download MendeleyEfficient synthesis of tert-butyl 3-cyano-3-cyclopropyl-2-oxopyrrolidine-4-carboxylates: Highly functionalized 2-pyrrolidinone enabling access to novel macrocyclic Tyk2 inhibitors.
Sasaki, Y., Tokuhara, H., Ohba, Y., Okabe, A., Nakayama, M., Nakagawa, H., Skene, R., Hoffman, I., Zou, H., Yoshida, M.(2020) Bioorg Med Chem Lett 30: 126963-126963
- PubMed: 31980341
- DOI: https://doi.org/10.1016/j.bmcl.2020.126963
- Primary Citation of Related Structures:
6OVA - PubMed Abstract:
Herein we report an efficient method for the synthesis of a highly functionalized 2-pyrrolidinone, tert-butyl 3-cyano-3-cyclopropyl-2-oxopyrrolidine-4-carboxylate, from readily available starting materials. Utility of this compound was demonstrated in the synthesis of a novel series of macrocyclic Tyk2 inhibitors, leading to the identification of a potent and selective macrocyclic Tyk2 inhibitor (26).
Organizational Affiliation:
Pharmaceutical Research Division, Takeda Pharmaceutical Company Limited, 26‑1, Muraoka‑Higashi 2‑chome, Fujisawa, Kanagawa 251‑8555, Japan. Electronic address: yusuke.sasaki@takeda.com.
