Abstract: The present invention discloses a method for preparation of Apremilast. ?-phthalimino vinylsulfones are reacted through the asymmetric addition reaction to form an addition product, and the drug of Apremilast can be obtained from the addition product through simple reactions. The method is a process for synthesizing Apremilast in a more efficient way.

Abstract: This invention provides a novel method for the preparation of 2,3-disubstituted -4-oxy-cyclopentan1-one compounds that are useful for the synthesis of prostaglandins and prostaglandin analogs of industrial relevance. The method comprises the metal-catalyzed asymmetric 1,4-conjugate addition of vinylboron compounds to 2-substituted -4-oxy-cyclopent-2-en-1-ones. This method relies on the use of less toxic, easily-handled reagents, and can be performed under milder conditions than offered by some conventional methods, affording 2,3-disubstituted-4-oxy-cyclopentan-1-one compounds enantio- and diastereoselectively, which are precursors to the said prostaglandin and prostaglandin analogs, in high yield.

Abstract: This invention provides a novel method for the preparation of 2,3-disubstituted-4-oxy-cyclopentan-1-one compounds that are useful for the synthesis of prostaglandins and prostaglandin analogs of industrial relevance. The method comprises the metal-catalyzed asymmetric 1,4-conjugate addition of vinylboron compounds to 2-substituted-4-oxy-cyclopent-2-en-1-ones. This method relies on the use of less toxic, easily-handled reagents, and can be performed under milder conditions than offered by some conventional methods, affording 2,3-disubstituted-4-oxy-cyclopentan-1-one compounds enantio- and diastereoselectively, which are precursors to the said prostaglandin and prostaglandin analogs, in high yield.

Abstract: The present invention proposes a chiral diene ligand, a fabrication method thereof and applications thereof. The chiral diene ligand is a bicyclo[2.2.1] diene ligand having structural specificity and high stability, which favors the bicyclo[2.2.1] diene ligand to take part in asymmetric transformations, particularly an asymmetric addition reaction involving a metal catalyst in a basic environment. Most of the products of the reactions implemented by the chiral diene ligands of the present invention have superior optical activity. The method of the present invention comprises a first oxidation step, a saponification step, a second oxidation step, a deprotonation step, and a cross-coupling step. The chiral diene ligand of the present invention is very suitable to be used in the fabrication or synthesis of various chemicals and medical products.

Abstract: The present invention proposes a chiral diene ligand, a fabrication method thereof and applications thereof. The chiral diene ligand is a bicyclo[2.2.1] diene ligand having structural specificity and high stability, which favors the bicyclo[2.2.1] diene ligand to take part in asymmetric transformations, particularly an asymmetric addition reaction involving a metal catalyst in a basic environment. Most of the products of the reactions implemented by the chiral diene ligands of the present invention have superior optical activity. The method of the present invention comprises a first oxidation step, a saponification step, a second oxidation step, a deprotonation step, and a cross-coupling step. The chiral diene ligand of the present invention is very suitable to be used in the fabrication or synthesis of various chemicals and medical products.

Abstract: A novel camphor-derived ?-amino alcohol compound is disclosed. The novel camphor-derived ?-amino alcohol compound can be used in asymmetric addition of organozinc to aromatic and aliphatic aldehydes, including linear aliphatic ones, thus generating corresponding secondary alcohols in high yields and enantiomeric excess.

Abstract: A method for preparing a propargylic alcohol catalyzed by 2-morpholinoisobornane-10-thiol (MITH) is disclosed, which includes reacting R1CHO with R2CCH in the presence of R3ZnR4 and MITH, wherein each of R1, R2, R3, and R4, independently, is optionally substituted alkyl, alkenyl, cycloalkyl, cycloalkenyl, alkylsilyl, heterocycloalkyl, heterocycloalkenyl, aryl, aryloxy, or heteroaryl. The method can give enantioenriched propargylic alcohols with good enantioselective at low loading of MITH.

Abstract: A novel camphor-derived ?-amino alcohol compound is disclosed. The novel camphor-derived ?-amino alcohol compound can be used in asymmetric addition of organozinc to aromatic and aliphatic aldehydes, including linear aliphatic ones, thus generating corresponding secondary alcohols in high yields and enantiomeric excess.

Abstract: A method for preparing a propargylic alcohol catalyzed by 2-morpholinoisobornane-10-thiol (MITH) is disclosed, which includes reacting R1CHO with R2CCH in the presence of R3ZnR4 and MITH, wherein each of R1, R2, R3, and R4, independently, is optionally substituted alkyl, alkenyl, cycloalkyl, cycloalkenyl, alkylsilyl, heterocycloalkyl, heterocycloalkenyl, aryl, aryloxy, or heteroaryl. The method can give enantioenriched propargylic alcohols with good enantioselective at low loading of MITH.

Abstract: Provided are an organic electroluminescence device having high luminous efficiency and a long emission lifetime, and a transition metal complex compound realizing the organic electroluminescence device. In the transition metal complex compound, three ligands are crosslinked with a crosslinking group having a saturated cyclic structure or a saturated polycyclic structure in a tripod manner. The organic electroluminescence device includes an organic thin film layer composed of one or multiple layers including at least a light emitting layer, the organic thin film layer being interposed between a pair of electrodes. In the organic electroluminescence device, at least one layer of the organic thin film layer contains the transition metal complex compound.

Abstract: Provided are an organic electroluminescence device having high luminous efficiency and a long emission lifetime, and a transition metal complex compound realizing the organic electroluminescence device. In the transition metal complex compound, three ligands are crosslinked with a crosslinking group having a saturated cyclic structure or a saturated polycyclic structure in a tripod manner. The organic electroluminescence device includes an organic thin film layer composed of one or multiple layers including at least a light emitting layer, the organic thin film layer being interposed between a pair of electrodes. In the organic electroluminescence device, at least one layer of the organic thin film layer contains the transition metal complex compound.