Search

Bicyclol, an innovative hepatoprotective drug, was approved by the Chinese National Medical Products Administration (NMPA) in 2001 to treat Hepatitis B and drug-induced liver injury. Two active metabolites of bicyclol have been identified as M2 and M3. To evaluate the impact on drug safety and efficacy of possible drug-drug interactions (DDIs) associated with these metabolites, a sufficient quantity of these metabolites is required. Herein, we report a concise novel route for the synthesis of M2 and M3 using the Suzuki-Miyaura coupling as the key step. Furthermore, we complete the gram-scale syntheses of M2 and M3. [ABSTRACT FROM AUTHOR]

( - )-Talaumidin (1) and ( - )-galbelgin (2) have been synthesized via 4-pentenoic acid as a starting material with the overall yield of about 17.8 and 16.9%, respectively. The key steps include Evans asymmetry anti-aldol reaction, TBS protection, hydroboration, oxidation, Friedel-Crafts arylation, etc. [ABSTRACT FROM AUTHOR]

Racemic 4-demethylenglerin A (1'), a simplified analog of the guaiane-type sesquiterpene englerin A (1), has been synthesized. The cyclic hydrocarbon core structure was built through modified Metz approach using epoxynitrile cyclization and direct Aldol reaction to prepare the precursor of RCM. The primary cytotoxicity test summarized that C4 methyl has marked impacts on the bioactivity.

Objective: To design and synthesize a series of squamosamide cyclic analogues and to test their antioxidation activity., Methods: Eleven 3-substituted indole-2-one derivatives were designed and synthesized through 9 steps with p-hydroxyphenylacetic acid as the starting material and their structures were confirmed by nuclear magnetic resonance and mass spectrometry., Results: Eleven compounds showed antioxidation activity and the activities of compounds 9 and 13 matches the positive control FLZ-52., Conclusion: Cyclic reconstruction with FLZ-52 as the lead compound have some antioxidation activity.

Neocnidilide 1, isolated from Apium graveleues L (Umbelliferae), has shown activity to inhibit the growth of mycotoxin-producing fungi. An efficient method for the synthesis of the racemic neocnidilide by the stereoselective reaction of hemiacetal 6 with n-BuMgBr has been developed.