The present invention relates to a chiral spiro phosphine-nitrogen-sulfur (PNS) tridentate ligand, preparation method and application thereof. The PNS tridentate ligand is a compound represented by Formula I or Formula II, their racemates, optical isomers, or catalytically acceptable salts thereof. The ligand has a primary structure skeleton characterized as a chiral spiro indan skeleton structure with a thio group. The chiral spiro phosphine-nitrogen-sulfur tridentate ligand can be synthesized by reacting racemic or optical active compound 7-diary/alkyl phosphine-7-amino-1,1-spiro-dihydro-indene compound having a spiro-dihydro-indene skeleton as the starting material. The chiral spiro PNS tridentate ligand being complex with transition metal salt can be used in an asymmetric catalytic hydrogenation reaction for catalyzing carbonyl compound. In particular, in asymmetric hydrogenation reaction process, being complex with iridium for catalyzing -alkyl--keto ester can obtain a high catalytic activity (a catalyst amount of 0.0002% mol) and high enantioselectivity (up to 99.9% ee) result. So the present invention has a practical value for industrial and commercial production.

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The disclosure provides a process for the preparation of 3-(4-annitophenyl)-2-metlioxypropionic acid, and analogs and intermediates thereof, contemplated to be capable of modulating the activity of receptors, e.g., PPARs receptors.

The disclosure provides a process for the preparation of 3-(4-annitophenyl)-2-metlioxypropionic acid, and analogs and intermediates thereof, contemplated to be capable of modulating the activity of receptors, e.g., PPARs receptors.

Objects of the present invention are to provide an industrially applicable method for producing an optically active -amino acid in high yield and in a highly enantioselective manner, to provide a simple production method of an optically active ,-disubstituted -amino acid, and to provide an intermediate useful for the above production methods of an optically active -amino acid and an optically active ,-disubstituted -amino acid. The present invention provides a production method of an optically active -amino acid or a salt thereof, the production method comprising introducing a substituent into the carbon in the -amino acid moiety of a metal complex represented by the following Formula (1): ##STR00001##
by an alkylation reaction, an aldol reaction, the Michael reaction, or the Mannich reaction, and releasing an optically pure -amino acid enantiomer or a salt thereof by acid decomposition of the metal complex.

Objects of the present invention are to provide an industrially applicable method for producing an optically active -amino acid in high yield and in a highly enantioselective manner, to provide a simple production method of an optically active ,-disubstituted -amino acid, and to provide an intermediate useful for the above production methods of an optically active -amino acid and an optically active ,-disubstituted -amino acid. The present invention provides a production method of an optically active -amino acid or a salt thereof, the production method comprising introducing a substituent into the carbon in the -amino acid moiety of a metal complex represented by the following Formula (1): ##STR00001##
by an alkylation reaction, an aldol reaction, the Michael reaction, or the Mannich reaction, and releasing an optically pure -amino acid enantiomer or a salt thereof by acid decomposition of the metal complex.

Objects of the present invention are to provide an industrially applicable method for producing an optically active -amino acid in high yield and in a highly enantioselective manner, to provide a simple production method of an optically active ,-disubstituted -amino acid, and to provide an intermediate useful for the above production methods of an optically active -amino acid and an optically active ,-disubstituted -amino acid. The present invention provides a production method of an optically active -amino acid or a salt thereof, the production method comprising introducing a substituent into the carbon in the -amino acid moiety of a metal complex represented by the following Formula (1): ##STR00001##
by an alkylation reaction, an aldol reaction, the Michael reaction, or the Mannich reaction, and releasing an optically pure -amino acid enantiomer or a salt thereof by acid decomposition of the metal complex.

The invention features methods and compositions for the synthesis of multimerizing agents.

The invention features methods and compositions for the synthesis of multimerizing agents.

The invention features methods and compositions for the synthesis of multimerizing agents.

Provided are processes for the preparation of (S)-tert-butyl 4,5-diamino-5-oxopentanoate, or a salt, solvate, hydrate, enantiomer, mixture of enantiomers, or isotopologue thereof. Also provided are solid forms of various intermediates and products obtained from the processes.