C07C205/53

Asymmetrically catalyzed synthesis method of nitropyrazole amide compound
10464899 · 2019-11-05 ·

A synthesis method of -nitropyrazole amide compound through asymmetrical catalyzing technique is provided, a nitroalkane and an ,-unsaturated pyrazole amide are applied as the raw material, a complex formed by a chiral amine oxide with a rare earth metal compound is served as the catalyst, a 4 molecular sieve is served as an additive, the -nitropyrazole amide compound can be obtained with a yield more than 99% and enantiomeric excess more than 99% ee. The catalytic system not only has the advantages of simple operation, mild reaction conditions, requiring no acid/base additives, convenient product purification, high yield and enatioselectivity, compliance with green atomic economy, and promising prospects for industrial application, but also allows the obtained -nitropyrazole amide compound to undergo some simple chemical conversions to produce some molecules having physiological activities.

Asymmetrically catalyzed synthesis method of nitropyrazole amide compound
10464899 · 2019-11-05 ·

A synthesis method of -nitropyrazole amide compound through asymmetrical catalyzing technique is provided, a nitroalkane and an ,-unsaturated pyrazole amide are applied as the raw material, a complex formed by a chiral amine oxide with a rare earth metal compound is served as the catalyst, a 4 molecular sieve is served as an additive, the -nitropyrazole amide compound can be obtained with a yield more than 99% and enantiomeric excess more than 99% ee. The catalytic system not only has the advantages of simple operation, mild reaction conditions, requiring no acid/base additives, convenient product purification, high yield and enatioselectivity, compliance with green atomic economy, and promising prospects for industrial application, but also allows the obtained -nitropyrazole amide compound to undergo some simple chemical conversions to produce some molecules having physiological activities.

NEW PROCESSES AND INTERMEDIATES FOR NEP INHIBITOR SYNTHESIS

The present invention relates to a new chemical synthesis, intermediates and catalysts useful for the preparation of the neprilysin (NEP) inhibitor sacubitril, inter alia via nitro 5 compounds. It further relates to new intermediate compounds and their use for said new chemical synthesis route, as well as a new catalyst ligand.

NEW PROCESSES AND INTERMEDIATES FOR NEP INHIBITOR SYNTHESIS

The present invention relates to a new chemical synthesis, intermediates and catalysts useful for the preparation of the neprilysin (NEP) inhibitor sacubitril, inter alia via nitro 5 compounds. It further relates to new intermediate compounds and their use for said new chemical synthesis route, as well as a new catalyst ligand.

Palladium(II)-silica supported catalyst

A solid-supported palladium(II) complex which catalyzes the Mizoroki-Heck coupling reaction efficiently and a method of employing the solid-supported palladium(II) complex to synthesize cinnamic acid and derivatives thereof. The solid-supported palladium(II) complex is also stable and can be recycled without significantly losing catalytic activity.

Palladium(II)-silica supported catalyst

A solid-supported palladium(II) complex which catalyzes the Mizoroki-Heck coupling reaction efficiently and a method of employing the solid-supported palladium(II) complex to synthesize cinnamic acid and derivatives thereof. The solid-supported palladium(II) complex is also stable and can be recycled without significantly losing catalytic activity.