C07C271/22

OXA-SPIRODIPHOSPHINE LIGAND AND METHOD FOR ASYMMETRIC HYDROGENATION OF alpha, beta-UNSATURATED CARBOXYLIC ACIDS
20210340168 · 2021-11-04 ·

The present invention provides an oxa-spirodiphosphine ligand having a structure of general Formula (I) below:

##STR00001##

wherein in general Formula (I), R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same, and are alkyl, alkoxy, aryl, aryloxy, or hydrogen, in which R.sup.1, R.sup.2, R.sup.3 and R.sup.4 may or may not form a ring, any two of them may form a ring, or a polycyclic ring may be formed between two pairs of them; R.sup.5 and R.sup.6 is alkyl, aryl, or hydrogen; and R.sup.7 and R.sup.8 is alkyl, benzyl, or aryl. The present invention also provides a method for asymmetric hydrogenation of α,β-unsaturated carboxylic acids. A complex of the oxa-spirodiphosphine ligand with ruthenium shows excellent activity and enantioselectivity in the asymmetric hydrogenation of various α,β-unsaturated carboxylic acids, with which a chiral carboxylic acid product can be obtained with an enantioselectivity up to 99%.

OXA-SPIRODIPHOSPHINE LIGAND AND METHOD FOR ASYMMETRIC HYDROGENATION OF alpha, beta-UNSATURATED CARBOXYLIC ACIDS
20210340168 · 2021-11-04 ·

The present invention provides an oxa-spirodiphosphine ligand having a structure of general Formula (I) below:

##STR00001##

wherein in general Formula (I), R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same, and are alkyl, alkoxy, aryl, aryloxy, or hydrogen, in which R.sup.1, R.sup.2, R.sup.3 and R.sup.4 may or may not form a ring, any two of them may form a ring, or a polycyclic ring may be formed between two pairs of them; R.sup.5 and R.sup.6 is alkyl, aryl, or hydrogen; and R.sup.7 and R.sup.8 is alkyl, benzyl, or aryl. The present invention also provides a method for asymmetric hydrogenation of α,β-unsaturated carboxylic acids. A complex of the oxa-spirodiphosphine ligand with ruthenium shows excellent activity and enantioselectivity in the asymmetric hydrogenation of various α,β-unsaturated carboxylic acids, with which a chiral carboxylic acid product can be obtained with an enantioselectivity up to 99%.

NEPRILYSIN INHIBITORS

In one aspect, the invention relates to compounds having the formula:

##STR00001## where R.sup.1-R.sup.6, a, b, and Z are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.

NEPRILYSIN INHIBITORS

In one aspect, the invention relates to compounds having the formula:

##STR00001## where R.sup.1-R.sup.6, a, b, and Z are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.

NOVEL AMINO ACID DERIVATIVES

A novel amino acid derivative is provided, wherein the amino acid derivative is expected to improve binding affinity of polypeptides comprising the derivative therein.

NOVEL AMINO ACID DERIVATIVES

A novel amino acid derivative is provided, wherein the amino acid derivative is expected to improve binding affinity of polypeptides comprising the derivative therein.

AN IMPROVED PROCESS FOR THE PREPARATION OF SEMAGLUTIDE SIDE CHAIN

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The present invention relates to an improved process for the preparation of a compound of Formula (1), The invention also provides improved processes for the preparation of intermediates used in the synthesis of Formula (1). The compound of Formula (1) is used in the synthesis of Semaglutide.

AN IMPROVED PROCESS FOR THE PREPARATION OF SEMAGLUTIDE SIDE CHAIN

embedded image

The present invention relates to an improved process for the preparation of a compound of Formula (1), The invention also provides improved processes for the preparation of intermediates used in the synthesis of Formula (1). The compound of Formula (1) is used in the synthesis of Semaglutide.