abstract |
NEW MATERIAL:Compounds expressed by formula I [R is phosphono, -ZR 6 (Z is 1W6C alkylene; R 6 is carboxyl, etc.), etc., R 1 WR 4 are -COR 7 (R 7 is 1W30C linear alkyl substitutable with OH) or formula II (n 2 is 1W20), etc.; R 5 is H, phosphono, etc.; provide that, except combinations of R=phosphono, -ZR 6 and R 5 =H and phosphono, R 1 WR 4 =-COR 7 ] and salts thereof. n EXAMPLE: Carboxymethyl 2-deoxy-6-O-(2-deoxy-3-O-(N-dodecanoylglycyl)-4-O-phos- phono-2-tetradecanoylamino-β-D-glucopyranosyl]-3-O-tetradecaonyl-2- tetradecanoyl- amino-α-D-glucopyranoside. n USE: Antineoplastic agent with low toxicity. n PREPARATION: A compound of formula III [R 9 is OH-protecting group; R 10 is expressed by formula IV (R 13 is phosphono-protecting group), etc.; R 11 , R 21 and R 31 are -COR 71 (R 71 is 1W30C alkyl substitutable with protecting OH), etc.; R 12 is R 13 ; R 51 is H, etc.] is catalytically reduced in the presence of Pd/C catalyst, etc., in an atmosphere of hydrogen. n COPYRIGHT: (C)1989,JPO&Japio |