Patent ID: 7388083

Claim:
A method of producing 4′-keto-N-Trifluoroacetyl-4-R 1 daunorubicin having a formula represented by Formula (3), wherein R 1 is H, OH, or OMe, comprising: (a) reacting N-Trifluoroacetyl daunorubicin having a formula represented by Formula (2), wherein R 1 is H, OH or OMe, with AcX activated DMSO in aprotic solvent, wherein AcX=PySO 3 , SOCl 2 , PHal 3 , POHal 3 ; Hal=Cl, Br Ac=AlkCO; OC—(CH 2 ) n —CO, n=0÷4; AlkSO 2 ; ArCO; ArSO 2 Alk=alkyl of halogenalkyl radical, Ar=phenyl or substituted phenyl radical, X=Cl, Br, I, OAc; and Aprotic Solvent=DMSO, DMAA, HMPA, Acetonitrile, DCM and other halogenalkanes, aromatic hydrocarbons and mixtures thereof, to produce an intermediate sulfoxy salt represented by Formula (8), (b) reacting the intermediate sulfoxy salt represented by Formula (8) with a strong base tertiary amine to produce the 4′-keto-N-Trifluoroacetyl-4-R 1 daunorubicin of Formula (3), wherein said strong bases utilized for decomposition of the intermediate, Formula (8), are tertiary amines represented by the formula NR 9 R 10 R 11 , wherein R 9 , R 10 , R 11 =alkyl [C n H 2n+2 n=1-8] or cycloalkyl [C n H 2n n=4-7]; and R 10 , R 11 =—(CH 2 ) n —n =3-6.