Zheijiang Jiuzhou Pharmaceutical Co., Ltd.

Nankai University

Zhejiang Jiuzhou Pharmaceutical Co., Ltd.

Shoufei Zhu

Qilin Zhou

Lixin Wang

Shen Li

Wei Sun

Kun Li

Yanbo Yu

Huawei Liu

Mingyao Huang

Canming Zhang

Ling Dang

Xinyu Zhang

Wentao Li

Song Song

The present invention relates to cyclopropane skeleton monophosphine ligands and preparation methods for palladium complexes thereof and an application. Specifically, trans-diaryl substituted cyclopropane skeleton monophosphine ligands are synthesized after trans-1,2-diaryl ethylene undergoing the steps of cyclopropanation reaction, debromination reaction, substitution reaction, and the like. Palladium complexes prepared by coordinating the cyclopropane skeleton monophosphine ligands with a palladium salt show very high activity in catalyzing C—N bond coupling reactions, and have good application prospects.

Cyclopropane skeleton monophosphine ligands, palladium complexes thereof, preparation methods and application

The present invention relates to a spirobenzylamine-phosphine, preparation method therefor and use thereof. The compound has a structure represented by formula (I), wherein n=0 to 3; R, R, R, R, R, R, R, Rand Rhaving a value as defined in claim. Starting from the substituted 7-trifluoromesyloxy-7'-diarylphosphino-1,1&#x2032;-spiro-dihydroindene, the compound is synthesized in a two-step or three-step reactions. The new spirobenzylamine-phosphine is complexed with an iridium precursor and is subjected to ion exchange, to give an Iridium/spirobenzylamine-phosphine complex comprising various anions. The spiro benzyl amine-phosphine/Iridium complex according to the present invention may be used for catalyzing asymmetry hydrogenation of a variety of alpha-substituted acrylic acids, has high activity and enantio-selectivity, and has a good prospect of industrialization. 

Spirobenzylamine-phosphine, preparation method therefor and use thereof

The present invention relates to a preparation method of carboxylic acids with optical activity, particularly, publishes that very useful chiral carboxylic acids can be obtained by the asymmetric catalytic hydrogenation of tri-substituted &#x3b1;,&#x3b2;-unsaturated carboxylic acids, with the complexes of the chiral phosphor nitrogen ligands and iridium used as the catalysts which show high activity and enantioselectivity (up to 99.8% ee), thus provides a more efficient method with higher enantioselectivity for asymmetric catalytic hydrogenation of chiral carboxylic acid-like compounds, and has important application value to asymmetric hydrogenation of chiral carboxylic acids.

Application of iridium complexes in asymmetric catalytic hydrogenation of unsaturated carboxylic acids

The present invention belongs to a spiro phosphine-oxazoline and preparation method and application thereof, particularly, publishes a novel spiro phosphine-oxazoline and the preparation method of its iridium complex. The substituted 7-diaryl phosphino-7'-carboxy-1,1&#x2032;-Lo-dihydro-indene is used as the starting raw material to synthesize the novel spiro phosphine-oxazoline of the present invention through a two-step reaction. The novel spiro phosphine-oxazoline and the iridium precursor are complexed to become a complex, and then through ion exchange, an iridium/phosphine spiro-oxazoline complex with different anions can be obtained. The present invention overcomes the shortcomings of the existing technology. The cheap readily available amino alcohol is used as the raw material to synthesize the novel spiro phosphine-oxazoline, on the fourth position of the oxazoline ring of which there is no substitutent. The iridium complex of this novel spiro phosphine-oxazoline can catalyze the asymmetric hydrogenation of &#x3b1;-substituted acrylic acid, and shows very high activity and enantioselectivity, therefore has a very high research value and an industrialization prospect.

Spiro phosphine-oxazoline, preparation method and application thereof

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Trianjin, China

Shoufei Zhu