The present invention provides a method in which when using (+)-dibenzoyl-D-tartaric acid to optically divide (±)-1-methyl-4-(2,4,6-trimethoxyphenyl)-3-piperidinone, an ether-based solvent is added and an extremely high yield of (R)-1-methyl-4-(2,4,6-trimethoxyphenyl)-3-piperidinone (+)-dibenzoyl-D-tartrate is thereby obtained, a slurry thereof is treated with a base, a “three-dimensionally bulky reducing agent” is subsequently used, and cis-(−)-flocinopiperidol is thereby produced with surprisingly high selectivity.

The present invention relates to the design and synthesis of a class of novel chiral phosphine ligand, 1,2-bis(diphenylphosphinoalkylamido)-1,2-disubstituted ethane, and use in asymmetric catalytic reactions, such as asymmetric catalytic synthesis of pyrazoline-5-one with a chiral quaternary carbon center, i.e., highly enantioselective synthesis of 3-methyl-4-benzyl-4-(2-butyl-2,3-butadienyl)pyrazoline-5-one by using 3-methyl-4-benzylpyrazoline-5-one and benzyl (2-butyl-2,3-butadienyl) carbonate with tris(dibenzylideneacetone)dipalladium-chloroform adduct and this novel ligand as catalysts. The ligand designed by this present invention has the following advantages: the structure is novel, the synthesis and enlarge are simple, the enantioselective control effect in the practical reaction is excellent, which has a broad application prospect in chiral catalysis.

Arene-immobilized Ru(II)TsDPEN Noyori-Ikariya catalysts anchored to silica through the coordinated η6-arene are provided. The catalysts efficiently catalyze many reactions, including the asymmetric transfer hydrogenation of ketones to alcohols.

The present invention relates to novel processes for the enantioselective iridium-catalysed hydrogenation of oximes and oxime ethers to provide compounds of formula (II) and salts thereof formula (I) and (II).

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In one aspect, the disclosure relates to substituted axially-chiral cannabinol analogs, methods of making same, pharmaceutical compositions comprising same, and methods of treating pain using same. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present disclosure.

In one aspect, the disclosure relates to substituted axially-chiral cannabinol analogs, methods of making same, pharmaceutical compositions comprising same, and methods of treating pain using same. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present disclosure.

Provided herein are enantioselective organocatalytic methods for preparing chiral tetraaryl methanes.

Provided herein are enantioselective organocatalytic methods for preparing chiral tetraaryl methanes.

Disclosed herein are antimicrobial compounds compositions, pharmaceutical compositions, the method of use and preparation thereof. Some embodiments relate to boronic acid derivatives and their use as therapeutic agents, for example, β-lactamase inhibitors (BLIs).

The present invention relates to an improved asymmetric synthesis of alpha-branched amines (hereafter referred to as the compound) and relative chiral amines (1″) or its pharmaceutically acceptable salt and derivatives. The process comprises an unusual substrate specific regioselective ortho lithiation of substituted arene compounds, followed by its highly diastereoselective addition to N-tert-butanesulfinylimines resulting in the selective formation of alpha-branched sulfinyl amine and chiral amine; which on subsequently removing the sulfinyl group provides corresponding alpha-branched amines or relative chiral amines (1″).