Sakamoto S, Tsuchiya T, Tanaka A, Umezawa S, Hamada M, Umezawa H
J Antibiot (Tokyo). 1985 Apr;38(4):477-84. doi: 10.7164/antibiotics.38.477.
23-Amino-4',23-dideoxymycaminosyl tylonolide diethyl acetal (5) has been prepared from 4',23-dideoxy-23-iodomycaminosyl tylonolide diethyl acetal (3) by treatment with sodium azide followed by selective reduction of the resulting azide (4). 23-Acylamino-23-deoxy (6 approximately 8) and 23-deoxy-23-urethane-type compounds (12 approximately 15) were further prepared. Treatment of the 23-alkylamino-4',23-dideoxymycaminosyl tylonolides (9, 10) with chloroformates gave 23-N-alkyl-23-deoxy-23-urethane-type compounds (16 approximately 21, 29, 30). 23-N-Alkyl-23-deoxy-23-(2-hydroxyethalamino and 2-methoxyethylamino)-4',23-dideoxymycaminosyl tylonolides (22 approximately 25, 27, 28) were prepared from 3 and the corresponding amines. Antibacterial activities and toxicities (for 23 and 27) of these compounds are described. toxicities (for 23 and 27) of these compounds are described.
23-氨基-4',23-二脱氧霉胺糖基泰洛内酯二乙缩醛（5）由4',23-二脱氧-23-碘霉胺糖基泰洛内酯二乙缩醛（3）经叠氮化钠处理，随后对生成的叠氮化物（4）进行选择性还原制得。进一步制备了23-酰基氨基-23-脱氧（6至8）和23-脱氧-23-脲酯型化合物（12至15）。用氯甲酸酯处理23-烷基氨基-4',23-二脱氧霉胺糖基泰洛内酯（9,10）得到23-N-烷基-23-脱氧-23-脲酯型化合物（16至21、29、30）。由3和相应的胺制备了23-N-烷基-23-脱氧-23-(2-羟乙氨基和2-甲氧基乙氨基)-4',23-二脱氧霉胺糖基泰洛内酯（22至25、27、28）。描述了这些化合物的抗菌活性和毒性（针对23和27）。描述了这些化合物的毒性（针对23和27）。
