Highly potent inhibitors of TNF-α production. Part I
摘要:
Discovery of new chemical leads of inhibitors for TNF-alpha production starting from the chemical modification of I is reported. Further biological studies of 1 to disclose the site of its action strongly suggested that 1 inhibits LPS-induced TNF-alpha expression in the liver and spleen of mice. Structure-activity relationships (SARs) are also discussed and full details including the chemistry are reported. (C) 2002 Elsevier Science Ltd. All rights reserved.
Catalyzed by a rhodium complex of P-stereogenic diphosphine ligand trichickenfootphos (TCFP), asymmetric hydrogenation of racemic aldimines via dynamic kineticresolution has been realized for the preparation of chiral arylglycines with good yields and enantioselectivities.
Lawesson's reagent promoted deoxygenation of azlactones for the syntheses of 2,4-disubstituted thiazoles
作者:Gaofeng Yin、Xiaodong Wang、Yuqing Wang、Tao Shi、Yaofu Zeng、Yuying Wang、Xue Peng、Zhen Wang
DOI:10.1039/d2ob01939f
日期:——
Azlactones and thiazoles are common structural motifs and possess diverse applications. A new method for the efficient and straightforward syntheses of 2,4-disubstituted thiazoles from azlactones has been developed. The reaction proceeded via deoxygenation of azlactones by Lawesson's reagent without metal or external additives. A variety of 2,4-disubstituted thiazoles were synthesized with up to 92%