A process for preparing Anastrozole is provided. In the process the steps of a. combining 3,5-bis(2-cyanoisopropyl)toluene, a solvent selected from the group consisting of acetonitrile, dichloromethane and chlorobenzene, a brominating reagent selected from a group consisting of N-bromosuccinimide and 1,3-dibromo-5,5-dimethylhydantoin, and 2,2'-azobis(2-methylpropionitrile); b. heating; c. combining with 1,2,4-triazole, a solvent selected from a group consisting of N-methylpyrrolidinone, dimethylformamide, mixtures of NMP and DMF, dimethylsulfoxide, mixtures of DMSO and toluene, acetone, ACN, and tetrahydrofuran, a base selected from a group consisting of NaOH, KOH, K.sub.2CO.sub.3, and Na.sub.2CO.sub.3, and 1,3-benzendiacetonitrile-5-(bromomethyl)-.alpha.,.alpha.,{acute over (.alpha.)},{acute over (.alpha.)}-tetramethyl, at a temperature below -20.degree. C. are performed.

Sicor, Inc.

Process for the preparation of anticancer drugs

Antibiotic 81-484 of the following physico-chemical properties:(1) elementary analysis: C.sub.33 H.sub.48 O.sub.7 (high resolution mass spectrum);(2) molecular weight: 556 [Field desorption (FD) mass spectrum];(3) melting point: not clear (oily at 10.degree.-100.degree. C.);(4) specific rotation: [.alpha.].sub.D.sup.20 =-151.degree. (c=0.1, methanol);(5) ultraviolet absorption spectrum: shown in FIG. 1 (in methanol);(6) infrared absorption spectrum: shown in FIG. 2 (KBr tablet);(7) solubility: insoluble in hexane and water, soluble in diethyl ether, methanol, ethanol, dichloromethane, chloroform, ethyl acetate, butyl acetate, acetone and benzene;(8) nuclear magnetic resonance spectrum: shown in FIG. 3 (CDCl.sub.3, TMS);(9) nature: acidic substance;(10) color reaction:negative for ninhydrin, anthrone-H.sub.2 SO.sub.4 and ferric chloride reaction;positive for iodine and antimony trichloride;weakly positive for Zatkis reagent;or a non-toxic salt thereof, is produced by culturing Streptomyces 81-484 FERM-P 7371 in a culture medium, and isolating the thus-produced antibiotic therefrom. The antibiotic has no antibiotic activity against Gram-positive and -negative bacteria, has antimicrobial activity against some kinds of fungi, and has growth inhibitory activity against P388 mouse leukemia cells and sarcoma 180 cells.

dichloromethane/хорт хавдар

Process for the preparation of anticancer drugs

Antitumor antibiotic 81-484 and process for its production

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