The first enantioselective total syntheses of highly complex hexacyclic meroterpenoids STR-2 and -9 (strongylophorine (STR)) are reported. Key elements of the synthetic route include the use of Robinson-type annulation reaction to construct the tricyclic terpenoid building block and a highly efficient PIDA-mediated 1,3-diaxial sp3 C–H activation to incorporate the requisite δ-lactone moiety. This route
Substituted benzofuran, benzopyrrole, benzothiophene, and structurally related complement inhibitors
申请人:BioCryst Pharmaceuticals, Inc.
公开号:US11021458B2
公开(公告)日:2021-06-01
Disclosed are compounds of formulae I and II, and pharmaceutically acceptable salts and prodrugs thereof, which are inhibitors of the complement system. Also provided are pharmaceutical compositions comprising such a compound, and methods of using the compounds and compositions in the treatment or prevention of a disease or condition characterized by aberrant complement system activity.
公开了式 I 和 II 的化合物及其药学上可接受的盐和原药,它们是补体系统的抑制剂。还提供了包含此类化合物的药物组合物,以及使用这些化合物和组合物治疗或预防以补体系统活性异常为特征的疾病或病症的方法。
WO2019195720A5
申请人:——
公开号:WO2019195720A5
公开(公告)日:2022-04-13
Counterattack Mode Differential Acetylative Deprotection of Phenylmethyl Ethers: Applications to Solid Phase Organic Reactions
作者:Asit K. Chakraborti、Sunay V. Chankeshwara
DOI:10.1021/jo801659g
日期:2009.2.6
A counterattack protocol for differential acetylative cleavage of phenylmethyl ether has been developed. The phenylmethyl moiety is liberated as benzyl bromide that is isolated and reused providing advantages in terms of waste minimization/utilization and atom economy. The applicability of this methodology has been extended for solid phase organic reactions with the feasibility of reuse of the solid support.
SUBSTITUTED BENZOFURAN, BENZOPYRROLE, BENZOTHIOPHENE, AND STRUCTURALLY RELATED COMPLEMENT INHIBITORS