| 摘要 |
A process for the preparation of 0-alkylated hydroxylamines of general formula (I) wherein X represents -OR', -SR' or ; R1 represents hydrogen or, if X is -OR1, an amino group, or alkyl or a mono- or binuclear optionally substituted aryl radical; R2 and R3 which may be the same or different each represents hydrogen, optionally substituted alkyl or cycloalkyl, aralkyl or diaralkyl or aryl, hydroxyl, if the other of R2 and R3 is hydrogen; or R2 and R3 together with the nitrogen atom to which they are attached represent an optionally substituted 5- to 7-membered saturated ring optionally interrupted by A further hetero atom or a 5-membered heteroaromatic ring optionally anellated with a benzene or uracil ring; together with their physiologically compatible acid addition salts with those organic or inorganic acids which permit the preparation of non-toxic salts, in which in a first state a hydroxylamine compound of formula (VII) (VII) is reacted with a compound of formula U-R6 (VIII) to form compounds of formula (IX) protecting groups are separated therefrom as by hydrolysis and the product of formula (I) is isolated in the form of a free base or is converted with a suitable acid into a physiologically compatible acid addition salt, wherein in the above formulae; R4 represents optionally substituted alkyl or aryl; R5' represents hydrogen, optionally substituted alkyl or aryl or halogen; R6 has the meanings specified above for y or additionally represents the radical ; T represents a hydrogen atom, if U has a different meaning from hydrogen, or the group or U represents a hydrogen atom, if T has a different meaning from hydrogen, or the group or and Z represents a halogen atom, or a reactive sulphonic acid ester group, whereby in each case T or U is hydrogen. |
