21092-94-4Relevant articles and documents
RAPAFUCIN DERIVATIVE COMPOUNDS AND METHODS OF USE THEREOF
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Paragraph 0480-0481, (2021/04/02)
The present disclosure provides macrocyclic compounds inspired by the immunophilin ligand family of natural products FK506 and rapamycin. The generation of a Rapafucin library of macrocyles that contain FK506 and rapamycin binding domains should have grea
Method for synthesizing houttuynine hybridized flavone Houttuynoid A
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Paragraph 0042; 0043, (2018/05/30)
The invention discloses a method for synthesizing houttuynine hybridized flavone Houttuynoid A. The method mainly comprises the following steps: by taking 3,4-dihydroxy benzaldehyde as an initiator raw material, firstly, selectively protecting four-position hydroxyl, performing an iodination reaction so as to obtain an o-iodophenol structure; further protecting aldehyde by using 1,3-propylene glycol, performing a Michael addition reaction with methyl-2-undecynoate so as to obtain an intermittent, and further performing an intracellular Heck reaction on the intermittent so as to obtain a key intermittent 2,3-di-substituted benzofuran structure; deprotecting the aldehyde of the benzofuran structure, performing a Claisen-Schmidt reaction with trihydroxyacetophenone monohydrate so as to obtaina chalcone structure, further performing iodine-catalyzed ring closure and DMDO (Dimethyldioxirane) oxidation so as to obtain a flavonol structure, furthermore removing a protection group, further reacting with bromo-peracetylated galactose so as to obtain glucoside, finally removing all protection groups, and performing reduction, thereby obtaining a target compound, namely the houttuynine hybridized flavone Houttuynoid A. Related derivatives are synthesized through intermittents of synthesis routs. The method is simple and controllable in reaction and high in yield.
NOVEL RENIN INHIBITOR
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Paragraph 0348; 0349; 0350, (2015/09/22)
The present invention provides a nitrogen-containing saturated heterocyclic compound of the formula [I] which is useful as a renin inhibitor. wherein R1 is a cycloalkyl group or an alkyl, R22 is an optionally substituted aryl and the like, R is a lower alkyl group, R3, R4, R5 and R6 are the same or different, and are a hydrogen atom, an optionally substituted carbamoyl, an optionally substituted alkyl, or alkoxycarbonyl, or a pharmaceutically acceptable salt thereof.