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ASUKAMYCIN DERIVATIVE, SYNTHESIS THEREOF AND CARCINOSTATIC AGENT
ASUKAMYCIN DERIVATIVE, SYNTHESIS THEREOF AND CARCINOSTATIC AGENT
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机译:阿司卡霉素衍生物,其合成及抗癌剂
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摘要
NEW MATERIAL:A compound expressed by formula I (R1 is amoinocarbonyl; R2 is H or tert-butyloxycarbonyl; R3 is H or two R3 groups together form isopropylidene, provided that R1 will not represent L-alanyl). EXAMPLE:N6-tert-Butyloxycarbonyl-2-chloro-9-[5'-O-(N-tertbut yloxycarbonyl-L- phenylalanyl)sulfamoyl-beta-D-ribofuranosyl]adenine. USE:A carcinostatic agent. PREPARATION:A compound expressed by formula II, e.g. N6-tert-butyloxycarbonyl-2-chloro-9-(2',3'-O-isopropylidene-5'-O-sul famoyl-beta-D-ribofurano syl)adenine, is reacted with di-tert-butyl dicarbonate to give a compound expressed by formula III, which is then reacted with an active ester of an aminocarboxylic acid (without including L-alanine).
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机译:新材料:由式I表示的化合物(R 1为氨基羰基; R 2为H或叔丁氧羰基; R 3为H或两个R 3基团一起形成异亚丙基,条件是R 1 >不会代表L-丙氨酰)。实施例:N 6-叔丁氧羰基-2-氯-9- [5'-O-(N-叔丁氧羰基-L-苯丙氨酰基)氨磺酰基-β-D-呋喃呋喃糖基]腺嘌呤。用途:抗癌剂。制备:由式II表示的化合物,例如使N 6-叔丁氧羰基-2-氯-9-(2',3'-O-异亚丙基-5'-O-磺酰酰基-β-D-呋喃呋喃基)基腺嘌呤与二-叔丁基反应。用二碳酸二丁酯得到式III表示的化合物,然后使其与氨基羧酸的活性酯(不包括L-丙氨酸)反应。
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