| 摘要 |
<p>PURPOSE:To provide a new methotrexate derivative useful as an anticancer agent. CONSTITUTION:A compound of formula I (R1 is CH2, CH2CH2, CH2O, CH2S, CH2SO, CH2SO2, CH2NH; R2 is H, 1-4C alkyl; n is an integer of 1-4; R3 is COOR4, NHCOR5, CONR6R7, PO3H2, SO3H; R4, R6 are H, 1-4C alkyl; R5, R7 are phenyl which may be substituted; R7 is 1-4C alkyl), e.g. N-[1-[2,4-diamino-6- pteridinyl)methyl]-indolinecarbonyl]-L-glutamic acid of formula II. The compound is obtained by reacting a compound of formula III (X is halogen) with a compound of formula IV in a solvent such as dimethylacetoamide at a temperature of 0-100 deg.C. When R2 is especially H, the compound is obtained by adding an IN sodium hydroxide solution to a solvent such as ethanol and stirring the mixture at a temperature of 0-60 deg.C. The compound of formula IV can be produced from a compound of formula V (A1 is protecting group) through three processes.</p> |
