2311-91-3Relevant academic research and scientific papers
Efficient synthesis of cholic acid derivates through stereoselective C–H functionalization from hyodeoxycholic acid
Liang, Yu-Yan,Huang, Huan,Li, Yang,Du, Rong-Kai,Li, Jing,Liu, Yong-Hong,Li, Shan,Zhang, Lei
, (2020)
Five cholic acid derivatives (including allo-ω-muricholic acid and CDCA) were synthesized from hyodeoxycholic acid via selective oxidation of C3- or C6-hydroxyl groups by IBX and NBS oxidants and stereocontrolled conversion. The hydroxyl group could be introduced through hydrolyzing α-Br keto with K2CO3 aqueous solution or through oxidizing the double bond by monoperoxyphthalic acid. The reduction of C6-O6 carbonyl to methylene could undergo with PTSH, NaBH3CN and ZnCl2 only at 5β configuration. A feasible synthetic route of CDCA from HDCA has been established to avoid the epimerization with the yield of 45% (8 steps). These strategies provided good yields, stereoselectivity and reproducibility for the preparation of cholic acid derivates and CDCA.
Fast Assembly and High-Throughput Screening of Structure and Antioxidant Relationship of Carotenoids
Kim, Dahye,Shi, Gaosheng,Kim, Yunji,Koo, Sangho
supporting information, p. 714 - 718 (2019/01/25)
C20 heptaenyl diphosphonate 4 was prepared for one-pot synthesis of carotenoids 1. Olefination with various aromatic aldehydes allowed fast assembly of the corresponding carotenoids. The SAR of carotenoids was investigated by high-throughput screening of ABTS and DPPH assays and their hierarchical clustering analysis. Antioxidant activity of carotenoids increased with the number of electron-donating substituents. Carotene 1a with multiple electron-donating substituents was most proficient, which showed better radical scavenging activities than β-carotene and lycopene.
Selective deoxygenation of allylic alcohol: Stereocontrolled synthesis of lavandulol
Kim, Hee Jin,Su, Liang,Jung, Heejung,Koo, Sangho
supporting information; experimental part, p. 2682 - 2685 (2011/06/26)
Selective deoxygenation of allylic alcohol can be successfully carried out by the formation of alkoxyalkyl ether (EE or MOM), followed by Pd(dppe)Cl 2-catalyzed reduction with LiBHEt3. (+)-S-Lavandulol has been efficiently synthesized by the application of this protocol to the diol derived from the Pb(OAc)4-promoted oxidative ring-opening of (-)-R-carvone. This deoxygenation method is general and selective for allylic alcohols.
N-ARYLSULFONYL-3-AMINOALKOXYINDOLES
-
Page 53, (2008/06/13)
The present invention describes substituted 3-Aminoalkoxyindoles, compounds of the general formula (I), its stereoisomers, its radioisotopes, its geometric forms, its N-oxides, its polymorphs, its pharmaceutically acceptable salts, its pharmaceutically acceptable solvates, its useful bio-active metabolites and any suitable combination of the above. The invention also discloses the processes for preparing such compounds of the general formula (I), its stereoisomers, its radioisotopes, its geometric forms, its N-oxides, its polymorphs, its pharmaceutically acceptable salts, its pharmaceutically acceptable solvates, its useful bio-active metabolites and also includes any suitable combination of the above. Further described are various methods of administering these compounds of general formula (I), i.e. pharmaceutically acceptable dosage forms, their composition and their use in either therapy or diagnosis.
N-ARYLALKYL-3-AMINOALKOXYINDOLES AND THEIR USE AS 5-HT LIGANDS
-
Page 44; 45, (2010/02/07)
The present invention describes substituted 3-Aminoalkoxyindoles, as compounds of the general formula (I), its stereoisomers, its radioisotopes, its geometric forms, its N-oxides, its polymorphs, its pharmaceutically acceptable salts, its pharmaceutically acceptable solvates, its useful bioactive metabolites and any suitable combination of the above. The invention also discloses the processes for preparing such compounds of the general formula (I), its stereoisomers, its radioisotopes, its geometric forms, its N-oxides, its polymorphs, its pharmaceutically acceptable salts, its pharmaceutically acceptable solvates, its useful bio-active metabolites and also includes any suitable combination of the above. Further described are various methods of administering these compounds of general formula (I), i.e. pharmaceutically acceptable dosage forms, their composition and their use in either therapy or diagnosis.
Crystal of bicalutamide and production method thereof
-
Page/Page column 11, (2008/06/13)
The present invention relates to a crystal of bicalutamide having a defined form, as well as economical and industrially practical production methods of bicalutamide and a crystal thereof, which are superior in environmental benignity and safety. Accordingly, the present invention provides a production method of bicalutamide represented by the formula (I): which includes at least a step of reacting a compound represented by the formula (3): with an oxidizing agent, a production method of a crystal of bicalutamide, as well as a crystal form of bicalutamide as defined by X-ray diffraction (XRD) or solid 13C NMR measurement.
Hydrolysis and First Ionization Constant of Monoperoxyphthalic Acid
Jones, Peter,Haggett, Max L.,Holden, Dennis,Robinson, Peter J.,Edwards, John O.,et al.
, p. 443 - 448 (2007/10/02)
The ionization constant for the carboxy proton of monoperoxyphthalic acid (MPPA) has been determined as 1.1 x 10-3, based on pKa1 2.96 +/- 0.05 at 21 deg C and ionic strength 0.024 mol dm-3 obtained by a distribution method.In the pH range 1 - 4 the observed rate constant for hydrolysis of MPPA increases by a factor of > 2 presumably as a result of intramolecular catalysis by the carboxylate function in the peroxy acid monoanion.At pH > 4, trace-impurity-induced decompositions of both MPPA and hydrogen peroxide prevented satisfactory studies of the hydolysis reaction.At pH 10+> ca. 0.7, and then increases rapidly with the onset of an acid-catalysed reaction at higher acidity.
