Novel derivative of 2-amino-2-[2-(4-octylphenyl)ethyl]-1,3-propandiol and application of novel derivative

[0019] Preparation of 2-amino-2-[2-(4-octylphenyl)-1,1-difluoroethyl]-1,3-propanediol.

[0020] The preparation of derivatives described in the present invention comprises 3 steps, and synthetic route is as follows:

[0021]

[0022] 1. Preparation of 2-bromo-2,2-difluoro-1-(4-octylphenyl)-ethanone 1-1 by acetylation.

[0023] Under anhydrous, oxygen-free and argon protection, aluminum trichloride, octylbenzene and anhydrous dichloromethane solvent were successively added to a dry flask at room temperature, and cooled to -10°C while stirring. A solution of 2-bromo-2,2-difluoro-acetyl bromide in dichloromethane was added and the mixture was allowed to come to room temperature and stirred overnight. The mixture was slowly poured into ice water, and the aqueous phase was extracted with dichloromethane, the combined organic layers were dried over anhydrous sodium sulfate, and concentrated under reduced pressure to give 2-bromo-2,2-difluoro-1-(4 -octylphenyl)-ethanone 1-1 was a b

[0029] Preparation of 2-amino-2-[2-(4-octylphenyl)-1-fluoroethyl]-1,3-propanediol.

[0030]

[0031]The preparation method is the same as in Example 1, except that 2-bromo-2,2-difluoro-acetyl bromide in Example 1 is replaced by 2-bromo-2-fluoro-acetyl bromide.

[0033] Preparation of 2-amino-2-[2-(4-octylphenyl)-1,1-difluoro-2,2-dideuterium-ethyl]-1,1,3,3-tetradeuterium-1, 3-Propanediol.

[0034]

[0035] The preparation method is the same as in Example 1, and the sodium borohydride in Example 1 is replaced with sodium borodeuteride.