| 摘要 |
Preparation of 4-(17 alpha -alkoxymethyl-17 beta -substituted-3-oxo-estra-4,9-dien-11 beta -yl)-benzaldehyde-(1E)-oxime urethane or (thio)carbonate derivatives (I) involves: (i) reacting oxime (II) with trichloromethyl chloroformate in presence of a tertiary amine; and (ii) reacting the obtained chlorocarbonate derivative (III) with a 1-7C alkyl or aryl alcohol (or thiol), an arylamine or a mono- or di-(1-7C alkyl)-amine. Preparation of 4-(17 alpha -alkoxymethyl-17 beta -substituted-3-oxo-estra-4,9-dien-11 beta -yl)-benzaldehyde-(1E)-oxime urethane or (thio)carbonate derivatives of formula (I) involves: (1) reacting the corresponding O-unsubstituted oxime of formula (II) with trichloromethyl chloroformate in a solvent in presence of a tertiary amine (preferably triethylamine) at -35 to +30 deg C; and (2) reacting the obtained chlorocarbonate derivative of formula (III) with a 1-7C alkyl or aryl alcohol, a 1-7C alkyl or aryl thiol, an arylamine or a mono- or di-(1-7C alkyl)-amine. R = NH2, OQ, OAr, SQ, SAr, NHQ, NHAr or N(Q)2; Q = 1-7C alkyl; R1 = H or 1-6C alkyl; R2 = 1-4C alkyl; and R3 = 1-6C alkyl.
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