METHOD OF PREPARING WATER-SOLUBLE CHLORINES Russian patent published in 2000 - IPC

FIELD: synthesis of biologically-active compounds. SUBSTANCE: new water-soluble chlorines that can find use as photosensitizers in photodynamic tumor therapy are prepared by interaction of initial chlorines with base solution. Initial chlorines are compounds with general formulas 1 or 2: (1) (2) wherein -CH(OAlk)CH₃, -CH=CH₂, -CHO, -C(O)CH₃ is R₂; R₃ hydrogen or lower alkyl; and -CH₃, methyl or aldehyde group. Bases involved in reaction can be linear or cyclic primary or secondary amines, amino acids, or amino acid salts. Initial chlorine is preliminarily reprecipitated by gradually adding water to its acetone solution. Stoichiometric quantity of base is directly added to wet chlorine precipitate, after which pH value of 1.5-2% aqueous solution of desired product is adjusted to 7.5-8.5 by adding concentrated solution of alkali or hydrochloric acid. Compounds are stable and fit to prepare injection solution. EFFECT: enlarged choice of antitumor agents. 2 cl, 4 tbl, 9 ex