C07C205/53

SOLID-SUPPORTED PALLADIUM(II) COMPLEX FOR CATALYZING MIZOROKI-HECK COUPLING REACTIONS AND A METHOD THEREOF

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.

PROCESS AND INTERMEDIATES FOR THE PREPARATION OF NEP INHIBITORS

The present invention relates to a new chemical synthesis, intermediates and catalysts useful for the preparation of the neprilysin (NEP) inhibitor sacubitril. It further relates to new intermediate compounds and their use for said new chemical synthesis route.

PROCESS AND INTERMEDIATES FOR THE PREPARATION OF NEP INHIBITORS

The present invention relates to a new chemical synthesis, intermediates and catalysts useful for the preparation of the neprilysin (NEP) inhibitor sacubitril. It further relates to new intermediate compounds and their use for said new chemical synthesis route.

Intermediate for synthesizing paroxetine, method for preparing the same, and uses thereof

A paroxetine intermediate, a method for preparing the same, and uses thereof are provided. Specifically, the method includes: reacting a compound of formula I below with a compound of formula II in the presence of an organic base under the catalysis of a complex formed from a chiral amine oxide L and a rare-earth metal compound Ln(OTf).sub.3 to prepare a compound of formula III below: wherein R.sub.1 is alkyl, phenyl or benzyl; R.sub.2, R.sub.3, R.sub.4 are each independently C.sub.1-C.sub.6 alkyl or C.sub.6-C.sub.10 aryl; the chiral amine oxide L has the following structure: wherein n=1, 2; and R=Ph, 2,6Me.sub.2C.sub.6H.sub.3, 2,6Et.sub.2C.sub.6H.sub.3, 2,6-iPr.sub.2C.sub.6H.sub.3, Ph.sub.2CH. ##STR00001##

ASYMMETRICALLY CATALYZED SYNTHESIS METHOD OF NITROPYRAZOLE AMIDE COMPOUND
20170291876 · 2017-10-12 ·

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.