Abstract: New ergoline derivatives are disclosed which are compounds of formula (I) having the structure: ##STR1## wherein R.sub.1 is hydrogen or methoxy; R.sub.2 is hydrogen or methyl; andX is hydroxy, R.sub.3 COO, S--R.sub.4 or NR.sub.5 R.sub.6 in which R.sub.3 is a straight or branched alkyl having from 1 to 6 carbon atoms, unsubstituted- or substituted-phenyl, the substituents being selected from the class consisting of chlorine, bromine, alkyl or alkoxy having from 1 to 4 carbon atoms, cycloalkyl containing from 3 to 6 carbon atoms, or a heterocycle;R.sub.4 is phenyl or a heterocycle, andR.sub.5 and R.sub.6 are alkyl having from 1 to 4 carbon atoms, or together with the N atom to which they are attached, forming a heterocycle.

Abstract: Optically active anthracyclinones are prepared by reacting an optically active (-) 1,4-dimethoxy-6-hydroxy-6-acetyl-tetralin with a phthalic anhydride in the presence of AlCl.sub.3 or AlBr.sub.3 and an alkali metal chloride at 130-180.degree. C. for 1 to 10 minutes.

Abstract: Racemic anthracyclinones of the general formula II ##STR1## when condensed with 2,3,6-trideoxy-3-trifluoroacetamido-4-0-trifluoroacetyl-.alpha.-L-lyxo-pyr anosyl chloride in the presence of silver trifluoromethane sulphonate yield an easily separable mixture of equimolar amounts of exclusively the .alpha.-glycoside of the 7S : 9S diastereomer and the .beta.-glycoside of the 7R : 9R diastereomer. In this way the biologically important .alpha.-glycosides of the 7S : 9S diastereomer of the general formula I (below) are easily prepared from a racemic anthracyclinone.

Abstract: Doxorubicin thioesters of the formula ##STR1## wherein R is acyl and which are useful in treating animal tumors, are prepared by reacting 14-bromo-daunomycin with a salt of a thioacid of the formula RSM wherein R is as defined above and M is an alkali metal atom or a quaternary ammonium salt in an inert polar solvent. The invention described herein was made in the course of work under a grant from the Department of Health, Education, and Welfare.

Abstract: Disclosed are optically active anthracyclinones and their daunosaminyl derivatives, which are useful for the treatment of malignant diseases, particularly sarcomas, breast cancer, bronchogenic carcinoma, malignant lymphomas, neuroblastomas, acute leukemia and bladder cancer.

Abstract: Daunomycin analogues of the formula: ##STR1## wherein when each R.sub.1 is hydrogen, each R is hydrogen, chlorine, bromine, methyl or methoxy and when each R.sub.1 is chlorine, bromine or methyl, each R is hydrogen, are useful in treating various mammalian tumors and are prepared by reacting a daunomycinone derivative of the formula: ##STR2## wherein R and R.sub.1 are as defined above with 1-chloro-2,3,6-trideoxy-3-trifluoroacetamido-4-trifluoroacetoxy-.alpha.-L- lyxopyranose in an inert anhydrous organic solvent in the presence of a catalyst and a hydrogen chloride acceptor.

Abstract: Disclosed are novel C-14 adriamycin esters which are useful in the treatment of certain tumors.

Abstract: 14-Aminodaunomycins, which are prepared by reacting 14-bromodaunomycin with an amine in a solvent at about 20.degree.-60.degree. C. are useful in treating certain tumors such as ascites Sarcoma 180 and solid Sarcoma 180.

Abstract: Anthracycline derivatives of the formula ##SPC1##Wherein R.sub.1, R.sub.2, R.sub. 3 and R.sub.4 are independently selected from the group consisting of hydrogen, chlorine, bromine and methoxy, with the proviso that at least one of the substituents is methoxy, and wherein R.sub.5 is selected from the group consisting of hydrogen, OH OR and OCOR; R being an alkyl group of 1 to 4 carbon atoms are prepared, in a single step, by selectively demethylating a compound of the formula: ##SPC2##Wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are as defined above by treating same with an aluminum halide in the presence of a suitable solvent at a temperature of 0.degree. to 50.degree.C.