PURPOSE: To obtain a novel compound which has biological activities such as antitumor action and can be efficiently synthesized from the stereospecific point of view.
CONSTITUTION: A compound of the formula I (R1 is H, halogen, lower alkyl; R2 is lower alkyl, allyl, alkinyl; R3 is halogen, H, OH; R4 is H, protecting group for OH; R6 is OH, amino) or its salt. The compound is obtained by allowing the compound of the formula II (Z is silyl OH-protecting group) to react with an organic acid such as pivalic acid and a halogenating agent such as N-bromo- succinimide to acyloxylation in the 1-position and halogenation in the 2'-position of the saccharide of the formula II, then allowing the resultant compound of formula III (R5 is acyloxy) to react, for example, with an organosilicon compound such as allyltrimethylsilane in the presence of a Lewis acid in a solvent such as methylene chloride to introduce a carbon substituent into the 1'-position in the saccharide, further, when needed, deprotecting the OH group and effecting amination in the 4-position.
TANAKA HIROMICHI
MIYASAKA SADA
YOSHIMURA YUICHI
KANOU FUMITAKA
