| 摘要 |
Phospholipid derivs. of formula - R1CH2-(CHR2)n-CH2OP(O)R3R4 (I) - and their salts are new (R1 is alkyl, alkoxy, alkylthio or alkylsulphonyl; R2 is H, OH, alkoxy, lower alkanoyloxy or lower alkylcarbamoyloxy; n is 0 or 1; R3 is opt. protected hydroxy; R4 is lower alkoxy or lower alicyclic-oxy both substd. with at least 2 opt. protected hydroxy gps. and opt. substd. by lower alkoxy or another alicyclic-oxy gp. substd. by at least 2 opt. protected hydroxy gps., the alicyclic ring opt. contg. O; lower is 1-6C and other alkyl etc. are 1-25C). - Specifically claimed are DL-2-O-Ethyl-3-O- octadecyl-glyceryl 2-(DL-myoinositol) phosphate and DL-2-O-methyl-3-O- octadecyl-glyceryl 1-(DL-chiro-inosityl) phosphate. - (I) have antitumour activity. Dose is 0.1-500 mg/kg, 1-4 times daily. USAB- US4585762 A New phospholipid derivs. have formula R1-CH2-(CH-R2)n-CH2-O-P(=O) -(R3)(R4) where R1 is higher alkyl or alkoxy; R2 is H, OH or lower alkoxy; n is 0 or 1; R3 is OH and R4 is lower alkoxy or lower alicyclic-oxy which is substd. with 2 or more OH and is opt. substd. with lower alkoxy. Pharmaceutically acceptable salts are also claimed. - A typical cpd. is DL-2-O-ethyl -3-O-octadecyl -glyceryl 2-(DL-myoinosityl) phosphate. Prepn. of cpds. (I) comprises reacting a cpd. of formula R1-CH2-(CH-Ra2)n-CH2-Y with a cpd. of formula X-P(=O)(Ra3)(Ra4) where X is halogen when Y is OH, or X is silver-oxy when Y is halogen, and Ra2 is H or alkoxy, Ra3 is protected OH and Ra4 contains protected OH gps.
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