FR-66973, FK-973

(1aS,3S,8R,9S,9aS)-1-乙酰基-7,9-二(乙酰氧基)-8-(((氨基羰基)氧基)甲基)-1,1a,2,8,9,9a-六氢-3,9-环氧-3H-氮丙啶并(2,3-c)苯并氮杂环辛四烯-5-甲醛 3,9-环氧-3H-阿锹铉[2,3-c][1]苯扎唑辛-5-羧醛,1-乙酰-7,9-双(乙酰氧)-8-[[(氨基羰基)氧]甲基]-1,1a,2,8,9,9a-六氢-(9CI) Chemical Name: [1aS-(1aalpha,3alpha,8alpha,9aalpha)]-7,9-Diacetoxy-1-acetyl-8-(carbamoyloxymethyl)-3,9-epoxy-5-formyl-1a,2,3,8,9,9a-hexahydro-1H-azirino[2,3-c][1]benzazocine; Carbamic acid (1aS,8R,9aS)-1-acetyl-5-formyl-7,9-diacetoxy-3,9-epoxy-2,3,8,9,9a,9b-hexahydro-1H-azirino[2,3-c][1]benzazocine-8-ylmethyl ester
CAS No. 114580-45-9, 113202-60-1 (error in MF)
项目整合开发状态: Phase II
项目研究机构: Fujisawa (Originator), Lyphomed (Originator)
合成路线:By acetylation of 8-carbamoyloxymethyl-5-formyl-7,9-dihydroxy-3,9-epoxy-1,1a,2,8,9,9a-octahydroazirino[2,3-c][1]benzazocine (FR-900482) (I) with acetic anhydride - pyridine.

合成路线:FR-900482 (I) was produced by culturing Streptomyces sandaensis No.6897 (FERM P-7654) and recovered by conventional methods.The acetylation of (I) with acetic anhydride gave the triacetyl derivative (II),which was selectively deacetylated with NaHCO3 in cool methanol yielding the diacetate (III).Finally,this compound was methylated by means of methyl iodide and K2CO3 in warm acetone.
📌 参考资料/链接:
参考文献标题:New tetracyclo cpds.,a process for their production and a pharmaceutical compsn.containing the same
文献作者:Kohsaka,M.; Terano,H.; Komori,T.; Iwami,M.; Yamashita,M.; Hashimoto,M.; Uchida,I.; Takase,S.(Fujisawa Pharmaceutical Co.,Ltd.)
参考来源:AU 8543728; EP 0166389; ES 8703477; ES 8707961; ES 8707962; JP 1986010590; JP 1989199975; JP 1995067623; US 4645765; US 4861774

📄 详细内容


合成路线:By acetylation of 8-carbamoyloxymethyl-5-formyl-7,9-dihydroxy-3,9-epoxy-1,1a,2,8,9,9a-octahydroazirino[2,3-c][1]benzazocine (FR-900482) (I) with acetic anhydride - pyridine.
参考文献标题:FK-973
文献作者:Hoshi,A.; Prous,J.; Castar,J.
参考来源:Drugs Fut 1989,14(2),119


产品链接: CAS No. 114580-45-9››

产品链接: CAS No.113202-60-1››