| 摘要 |
1-oxa-6-aza-cyclopentadecane-13,15-dione derivs. of formula (I) and their acid addn. salts are new. R1 and R2 are H or Me; Z is H or 1-18C acyl; R is alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, cycloalkynyl or 7-18C aralkyl. Also claimed are intermediates of formula (III)-(V) where M is a protecting gp. Specifically claimed (2R-(2R star,3S star,4R star,5R star,8R star,10R star,11R star,12S star,14R star)) -3,4-dihydroxy-2 -ethyl-3,5,6,8,12,14 -heptamehyl- 10-methoxy-11-(3,4,6- trideoxy- 3-dimethylamino -beta-D-xylohexopyranosyloxy) -1-oxa-6-aza- cyclopentadecane-13,15-dione (Ia). M is a protecting gp. In an example, treatment of (II; R = R1 = Me, R2 = H) with HCl gave the corresp. cpd. (III), which was reacted with Ac20 to give (IV; R = R1 = Me, R2 = H, M = Ac). The prod. (380mg) was suspended in 6ml CH2Cl2 together with 0.618 ml DMSO and 667 mg EDC. The mixt. was treated with 627mg pyridinium trifluoroacetate in 2ml CH2Cl, stirred for 30 mins. and worked up to give 200 mg (V; R = R1 = Me, R2 = H, M = Ac). This was stirred in 10 ml MeOH for 20 hr. to give 117 mg of prod. which was chromatographed to give (Ia).
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