112635-76-4Relevant articles and documents
A Concise Stereoselective Total Synthesis of Methoxyl Citreochlorols and Their Structural Revisions
Sunnapu, Ranganayakulu,Rajendar, Goreti
, p. 1637 - 1642 (2021/03/15)
A concise, stereoselective and protecting group free approaches for the total synthesis of (?)-(2S,4R)- and (+)-(2R,4S)-3′-methoxyl citreochlorols and their stereoisomers are demonstrated. All four stereoisomers were synthesized to establish the absolute stereochemistry of the reported structures and the structures were revised accordingly. The approach involves chelation controlled regioselective reduction of a diester, silyl iodide promoted ring-opening iodo esterification of lactones, highly chemo- and regioselective ring-opening of an epoxy ester, dichloromethylation of a carboxyl group, and syn- and anti-selective reduction of the resulted β-hydroxy ketone as key steps.
Design, Synthesis, and Evaluation of Tetrahydropyrrolo[1,2-c]pyrimidines as Capsid Assembly Inhibitors for HBV Treatment
Li, Xiaolin,Zhou, Kai,He, Haiying,Zhou, Qiong,Sun, Ya,Hou, Lijuan,Shen, Liang,Wang, Xiaofei,Zhou, Yuedong,Gong, Zhen,He, Shibo,Jin, Huangtao,Gu, Zhengxian,Zhao, Shuyong,Zhang, Long,Sun, Chunyan,Zheng, Shansong,Cheng, Zhe,Zhu, Yidong,Zhang, Minghui,Li, Jian,Chen, Shuhui
supporting information, p. 969 - 974 (2017/09/23)
The discovery of novel tetrahydropyrrolo[1,2-c]pyrimidines derivatives from Bay41-4109 as hepatitis B virus (HBV) inhibitors is herein reported. The structure-activity relationship optimization led to one highly efficacious compound 28a (IC50 = 10 nM) with good PK profiles and the favorite L/P ratio. The hydrodynamic injection model in mice clearly demonstrated the efficacy of 28a against HBV replication.
A new strategy for the synthesis of crucigasterin A, and cytotoxic activity of this compound and its related analogues
Kumar, Jayprakash Narayan,Reddy, Parigi Raghavendar,Das, Biswanath,Kumar, C. Ganesh,Sujitha, Pombala
, p. 5192 - 5194 (2013/09/12)
Stereoselective total synthesis of bioactive marine natural product crucigasterin A has been accomplished from commercially available and inexpensive l-(-)-malic acid as a starting material. Julia olefination and chelation controlled Grignard additions are the key steps involved in the present synthesis. Cytotoxic properties of crucigasterin A and its related analogues crucigasterins B and D have been evaluated. Crucigasterin A showed promising activities against both the human cervical cancer cell line and human breast adenocarcinoma cell line.