Method for synthesizing derivatives of chiral pyridyl aminoalcohols, and intermediate products and final products of same

The technology of an aromatic ring amino alcohol and a synthesis method, which is applied in the field of synthesis of derivatives, can solve the problems of low application value, difficult control of splitting conditions, and low purity (ee) value of easy racemic enantiomers of products, and achieves Inexpensive effect
CN101519374BActive Publication Date: 2013-05-15ASYMCHEM LAB TIANJIN +3
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
ASYMCHEM LAB TIANJIN
Publication Date
2013-05-15

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Abstract

The invention relates to a method for synthesizing the derivatives of chiral pyridyl aminoalcohols, and intermediate products and final products of the same. Initial materials are selected from commercial raw materials on the market or easy-to-prepare raw materials of halogenated pyridine alkyl ketone or aromatic ring ketones, wherein X is F or Cl, R1 is C1 to C8 alkyls or C3 to C8 cycloalkyls; and final products are obtained through a process of chemical reactions under mild conditions, wherein R1 is C1 to C8 alkyls or C3 to C8 naphthene base, R2 is H or C1 to C8 alkyls, or C3 to C8 cycloalkyls or C7 to C9 benzyls, and chiral centers of alcohols have an S or R structure. The method provides a new thought and means for preparing the derivatives of chiral pyridyl aminoalcohols; the intermediate products are that the chiral centers of alcohols have an S or R structure; and the final products are that the chiral centers of alcohols have an S or R structure.
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Description

(1) Technical field:

[0001] The invention relates to a synthesis method of derivatives of chiral pyridine aromatic ring amino alcohols and some intermediate products and final products thereof. (two) background technology:

[0002] Derivatives of chiral pyridine aromatic ring amino alcohols are introduced into peptide drugs to modify the peptide chain structure and enhance their stability and activity in living organisms; in addition, they can also be used as inhibitors or antioxidants to prevent such as Lung cancer, breast cancer, prostate cancer, arteriosclerosis and other malignant proliferative disorders, so as to achieve the purpose of treating cancer and tumor; for example, 1-S-(2-aminopyridin-3-yl)-1-propanol is In the synthesis of kinesin inhibitors for mitosis (drug patent EP1942899), such drug candidates are important drugs for the treatment of cell proliferative diseases.

[0003] At this stage, the methods for preparing such compounds mainly include the followin...

Claims

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