166170-15-6Relevant articles and documents
ALKYNYL QUINAZOLINE COMPOUNDS
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Paragraph 0738, (2021/02/19)
The present disclosure relates to compounds of Formula (I'): and pharmaceutically acceptable salts and stereoisomers thereof. The present disclosure also relates to methods of preparation these compounds, compositions comprising these compounds, and methods of using them in the prevention or treatment of abnormal cell growth in mammals, especially humans.
Synthetic method for novel chiral ligand, metal chelate, multiple unnatural amino acids, maraviroc and key intermediate thereof
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Paragraph 0204-0206, (2018/04/26)
The invention discloses a synthetic method for a novel chiral ligand, a metal chelate, multiple unnatural amino acids, maraviroc and a key intermediate thereof. According to the synthetic method, (R)-2-methylproline is selected as a starting material, and asymmetrical resolution is induced by utilizing a nickel chelate, so that (S)-beta3-amino acid is obtained, and (S)-3-amino-3-phenylpropionic acid is taken as the key intermediate for synthesizing maraviroc, so that yield is high, and ee value reaches more than or equal to 98.2%. The method disclosed by the invention has the advantages that source of raw materials is wide, conditions of a synthetic process are mild, control is easy, and optical purity of products is high.
Discovery of 2-alkyl-1-arylsulfonylprolinamides as 11β-hydroxysteroid dehydrogenase type 1 inhibitors
Yu, Jianxin,Liu, Haiyan,Xia, Guangxin,Liu, Lin,Xu, Zhenmin,Chen, Qian,Ma, Chen,Sun, Xing,Xu, Jiajun,Li, Hua,Li, Ping,Shi, Yufang,Liu, Xuejun,Shen, Jingkang,Xiong, Bing
supporting information, p. 793 - 798,6 (2020/09/15)
On the basis of scaffold hopping, a novel series of 2-alkyl-1- arylsulfonylprolinamides was discovered as 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD-1) inhibitors. A representative compound 4ek, obtained through SAR and structure optimization studies, demonstrates excellent in vitro potency against 11β-HSD-1 and dose-dependent in vivo inhibition of 11β-HSD-1 in a prednisone/prednisolone transformation biomarker study in mice.