Shenzhen Catalys Technology Co., Ltd.

Shenzhen Innovation Center of Small Molecule Drug Discovery Co., Ltd.

Xiaobing Ding

Qiwei Lang

Yang Xiao

Shuang Gao

Shaobai Yan

Disclosed are a chiral multidentate ligand (I), a preparation, and an application thereof. In this method, compound (M1) is subjected to condensation with compound (M2) followed by amine deprotection in the presence of a deprotection reagent to obtain compound (M4). Compound (1) is subjected to deprotonation by butyl lithium and phosphorization followed by dimethylamino group substitution to produce compound (3). The compound (3) and the compound (M4) are reacted in the presence of triethylamine to produce chiral multidentate ligands.

Chiral multidentate ligand, and application thereof in asymmetric hydrogenation

A method for preparing nicotine. (1) The nicotinic acid alkyl ester and N-methylpyrrolidone are subjected to a condensation reaction, and then added with a strong acid to obtain 4-methylamino-1-(3-pyridine)-butanone hydrochloride. (2) The 4-methylamino-1-(3-pyridine)-butanone hydrochloride is reacted with an amino-protecting reagent to obtain an intermediate (4). (3) A chiral alcohol (5) is obtained through an asymmetric reduction. (4) The chiral alcohol (5) is converted into the nicotine through a two-step reaction.

Method of asymmetrically synthesizing nicotine

The present invention relates to a preparation method of chiral primary amine. The chiral primary amine is prepared through a one-pot method that under the action of a ruthenium-chiral diphosphine catalyst, a simple ketone and an ammonium salt RCOONHhave reductive amination by adding hydrogen and then are heated and hydrolyzed by adding acid. The present invention has the advantages of good substrate universality, high reaction efficiency and the like

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Xiaobing Ding