| 摘要 |
Production of esterified colchinol phosphate derivatives (I) involves coupling a hydroxy-colchicine derivative (II) with a reactive phosphoric acid diester derivative (III) in presence of a compound (A) containing a non-aromatic amine function. Some compounds (I) are new. Production of esterified colchinol phosphate derivatives of formula (I) involves coupling a colchicine compound of formula (II) with a phosphoric acid derivative of formula R4-P(O)(OR1)(OR2) (III) in presence of a compound (A) containing a non-aromatic amine function. R1, R2 = optionally substituted alkyl or optionally substituted cycloalkyl, or R1 + R2 = optionally substituted alkylene or optionally substituted cycloalkylene, and R3, R4 = labile substituents. Independent claims are included for: (a) products (I) obtained by the present process; (b) (I; R1, R2 = halogenated aliphatic groups; or R1 + R2 = halogenated aliphatic group) as new compounds, provided that groups R1 and R2 are cleavable in presence of transition metal(s) to form a phosphate or phosphoric acid group; (c) the preparation of colchicinol phosphate (IV) (i.e. (I) with R1 and R2 replaced by H), by cleaving the groups R1 and R2 in (I) in presence of transition metal(s); (d) (IV) obtained by the present process; (e) the production of colchicinol phosphate salts (V) (i.e. (I) with R1 and R2 replaced by H, Li, Na or K, provided that at least one is Li, Na or K), by salifying (V) obtained by the present process with an alkaline compound containing a lithium, sodium or potassium cation; and (f) (V) obtained by the present process.
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