C07C231/18

Chiral spiro phosphorus-nirogen-sulphur tridentate ligand, preparation method and application thereof
10550138 · 2020-02-04 ·

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. ##STR00001##

Processes for the preparation of (<i>S</i>)-tert-butyl 4,5-diamino-5-oxopentanoate

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.

Processes for the preparation of (<i>S</i>)-tert-butyl 4,5-diamino-5-oxopentanoate

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.

Process of making 3-(4′-aminophenyl)-2-methoxypropionic acid, and analogs and intermediates thereof

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

Process of making 3-(4′-aminophenyl)-2-methoxypropionic acid, and analogs and intermediates thereof

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

Compositions and methods for preparing β,γ-unsaturated acids

The present disclosure provides methods for enantioselective synthesis of acyclic -quaternary carboxylic acid derivatives via iridium-catalyzed allylic alkylation.

Compositions and methods for preparing β,γ-unsaturated acids

The present disclosure provides methods for enantioselective synthesis of acyclic -quaternary carboxylic acid derivatives via iridium-catalyzed allylic alkylation.

Compositions and methods for preparing β,γ-unsaturated acids

The present disclosure provides methods for enantioselective synthesis of acyclic -quaternary carboxylic acid derivatives via iridium-catalyzed allylic alkylation.

PROCESSES FOR THE PREPARATION OF (S)-TERT-BUTYL 4,5-DIAMINO-5-OXOPENTANOATE

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.

PROCESSES FOR THE PREPARATION OF (S)-TERT-BUTYL 4,5-DIAMINO-5-OXOPENTANOATE

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.