Method for preparing tetrahydro-1-naphthylamine and derivatives thereof
AssigneesShanghai Senhui Medicine Co., Ltd., Jiangsu Hengrui Pharmaceuticals Co., Ltd.
InventorsWei JIANG, Qing HUANG, Junfeng GAO, Jian HUANG
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Abstract
The present disclosure relates to a method for preparing tetrahydro-1-naphthylamine and derivatives thereof. Specifically, the present disclosure relates to a method for preparing (1S,4S)-4-methoxy-1,2,3,4-tetrahydronaphthalen-1-amine, and the method comprises the step of reacting compound C-1 under the condition of (R)-2-methyl-CBS-oxazaborolidine so as to form compound D-1. The method is simple to operate and is suitable for industrial production.
Claims12
A method for preparing a compound represented by formula I or a salt thereof:
- comprising a step of reacting a compound represented by formula C in the presence of (R)-2-methyl-CBS-oxazaborolidine to form a compound represented by formula D,
- wherein R1 is selected from the group consisting of halogen, nitro, cyano, C1-6 alkyl, and C1-6 alkoxy, and the alkyl or alkoxy is optionally substituted with one or more groups selected from the group consisting of halogen, oxo, nitro, cyano, C1-6 alkyl, and C1-6 alkoxy;
- n is 0, 1, 2, or 3;
- R2 is selected from the group consisting of hydrogen, C1-6 alkyl, and C3-6 cycloalkyl, and the alkyl or cycloalkyl is optionally substituted with one or more groups selected from the group consisting of halogen, oxo, nitro, cyano, C1-6 alkyl, C1-6 alkoxy, and C3-6 cycloalkyl.
A compound represented by formula D or a pharmaceutically acceptable salt thereof:
- wherein R1 is selected from the group consisting of halogen, nitro, cyano, C1-6 alkyl, and C1-6 alkoxy, and the alkyl or alkoxy is optionally substituted with one or more groups selected from the group consisting of halogen, oxo, nitro, cyano, C1-6 alkyl, and C1-6 alkoxy;
- n is 0, 1, 2, or 3.
A compound represented by formula C or a pharmaceutically acceptable salt thereof:
- wherein R1 is selected from the group consisting of halogen, nitro, cyano, C1-6 alkyl, and C1-6 alkoxy, and the alkyl or alkoxy is optionally substituted with one or more groups selected from the group consisting of halogen, oxo, nitro, cyano, C1-6 alkyl, and C1-6 alkoxy;
- n is 0, 1, 2, or 3.
Dependencies are inferred from the claim text.