4838-96-4

Either aldehyde or cinnamyl ether products can be selectively extracted from raw sawdust by controlling the temperature and pressure of a solvolysis reaction. These materials have been used as platform chemicals for the synthesis of 15 different synthetic substrates. The conversion of the initial sawdust-derived materials into electron-rich aryl substrates often requires the use of oxidation and reduction chemistry, and the role electrochemistry can play as a sustainable method for these transformations has been defined.

Bridging the gap: The berberine bridge enzyme (BBE) was employed for the first preparative oxidative biocatalytic C-C coupling that leads to a new intramolecular bond. This unique transformation requires O2 as sole stoichiometric oxidant and gives access to novel optically pure (S)-berbine 2 and (R)-1-benzyl-1,2,3,4-tetrahydroisoquinoline 1 alkaloid derivatives by kinetic resolution.

A chemoenzymatic approach for the asymmetric total synthesis of the title compounds is described that employs an enantioselective oxidative C-C bond formation catalyzed by berberine bridge enzyme (BBE) in the asymmetric key step. This unique reaction yielded enantiomerically pure (R)-benzylisoquinoline derivatives and (S)-berbines such as the natural product (S)-scoulerine, a sedative and muscle relaxing agent. The racemic substrates rac-1 required for the biotransformation were prepared in 4-8 linear steps using either a Bischler-Napieralski cyclization or a C1-Cα alkylation approach. The chemoenzymatic synthesis was applied to the preparation of fourteen enantiomerically pure alkaloids, including the natural products (S)-scoulerine and (R)-reticuline, and gave overall yields of up to 20% over 5-9 linear steps.

The present invention relates to novel compounds of Formula (I), their pharmaceutically acceptable derivatives, tautomeric forms, stereoisomers including R and S isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The invention also rel

The present invention relates to an agent for treating nephritis and a TGF-β inhibiting agent comprising as an effective ingredient a pyridylacrylamide derivative represented by the following formula (I): wherein Ar1is a substituted or unsubstituted pyridyl group, Ar2is a substituted or unsubstituted phenyl group, R1is a hydrogen atom, an alkyl group or an aryl group, R2is a hydrogen atom, an alkyl group, a cyano group or an alkoxycarbonyl group, R3is a hydrogen atom or an optionally substituted alkyl group, X is an oxygen or sulfur atom, A and B are same or different and each represent a hydrogen atom, a hydroxyl group, an alkoxy group or an alkylthio group, or A and B together form an oxo or thioxo group, or a group represented by the formula: ═N—Y in which Y is a dialkylamino, hydroxyl, aralkyloxy or alkoxy group, or a group represented by the formula: —Z1—M—Z2— which Z1and Z2are same or different and each represent an oxygen or sulfur atom or an imino group optionally substituted by an alkyl group, and M is an alkylene group or a 1,2-phenylene group, or A is a hydroxyl group and B is a 1-alkylimidazol-2-yl group, and n is an integer of 1 to 3, or a pharmaceutically acceptable salt thereof; as well as the pyridylacrylamide derivatives.