88499-85-8Relevant articles and documents
Method for preparing chiral nitrogen-phosphorus ligand L-8 containing pyridocyclopentane
-
, (2021/03/23)
The invention discloses a method for preparing chiral nitrogen-phosphorus ligand L-8 containing pyridocyclopentane, and belongs to the technical field of medical intermediate chiral ligands. The chiral nitrogen-phosphorus L-8 ligand is prepared from cyclopentanone through the steps of addition, cyclization, chlorination, asymmetric boronation, oxidation, coupling, esterification and the like in sequence, large-scale preparation is relatively easy to achieve through the route, and the defect that in a traditional route, the yield is low in the first step of ring closing reaction and chiral alcohol preparation is overcome, and by selecting a proper chiral ligand, and combining with butyl lithium, asymmetric synthesis of chiral alcohol is realized, and a chiral separation column mode adoptedin literature is avoided.
SUBSTITUTED L,2-DIHYDRO-3H-PYRAZOLO[3,4-D]PYRIMIDIN-3-ONES
-
Paragraph 0156, (2019/10/01)
Compounds of Formula (I) are provided herein. Such compounds, as well as pharmaceutically acceptable salts and compositions thereof, are useful for treating diseases or conditions, including conditions characterized by excessive cellular proliferation, such as breast cancer.
Ligand-Enabled β-C–H Arylation of α-Amino Acids Without Installing Exogenous Directing Groups
Chen, Gang,Zhuang, Zhe,Li, Gen-Cheng,Saint-Denis, Tyler G.,Hsiao, Yi,Joe, Candice L.,Yu, Jin-Quan
, p. 1506 - 1509 (2017/02/05)
Herein we report acid-directed β-C(sp3)-H arylation of α-amino acids enabled by pyridine-type ligands. This reaction does not require the installation of an exogenous directing group, is scalable, and enables the preparation of Fmoc-protected unnatural amino acids in three steps. The pyridine-type ligands are crucial for the development of this new C(sp3)-H arylation.