公开(公告)号：US3505376A

公开(公告)日：1970-04-07

申请号：US3505376D

申请日：1965-10-22

申请人： YISSUM RES DEV CO

发明人： FRANKEL MAX ,  GERTNER DAVID ,  BROZE MORDECHAI ,  HANNA PARDESS ,  ZILKHA ALBERT

IPC分类号： C07F7/08 ,  C07F7/10

CPC分类号： C07F7/0818

摘要： Novel trialkylsilyl-b -phenylethylamine compounds having the formula wherein R1, R2 and R3 are alkyl, R4 is hydrogen, hydroxyl or alkyl, R5 is hydrogen, hydroxymethyl, carboxyl or alkyl, R6 and R7 are hydrogen or alkyl and when R6 is hydrogen then R7 may also be acyl or haloacyl, are prepared from intermediates of formula where n is 0 or 1, X is chlorine, carboxyl, nitrile or hydroxyl and R8 is hydrogen, alkyl or acyl. In examples preparations described are of b - (trimethylsilylphenyl)ethylamine from trimethylsilylbenzyl cyanide and lithium aluminium hydride; b -(trimethylsilylphenyl)ethyldimethylamine from b -(trimethylsilylphenyl)-ethyl chloride and dimethylamine; b -(trimethylsilylphenyl)-propylamine from a -(trimethylsilylphenyl)propionitrile and lithium aluminium hydride; 1-(trimethylsilylphenyl)-2-aminopropane by reacting trimethylsilylbenzyl cyanide with magnesium, then with methylcyanide and reducing with lithium aluminium hydride; b -(trimethylsilylphenyl) -serine from trimethylsilylbenzaldehyde and glycine; 1-(trimethylsilylphenyl)-2-aminopropane-1,3-diol from b -(trimethylsilylphenyl)serine and lithium aluminium hydride; 1 - (trimethylsilylphenyl) - 2 - dichloroacetamido propane-1,3-diol from the -2-aminopropane-1,3-diol and methyl dichloracetate. Intermediates, other than those used as starting materials above, which are prepared are trimethylsilylphenyl acetic acid, b -(trimethylsilylphenyl) ethyl alcohol, trimethylsilylbenzyl chloride and 1-cyano-1-(trimethylsilyl)-phenyl acetone. The methods of preparing the intermediates are described.