| 摘要 |
<p>3-R3-CH=CH- 4-R200C- 7-R1-NH 2 or 3-cephem derivs and their 1-oxides of formula (I) are new (where n is 0 or 1 and (A) R1 is a 2-R4NH-4-thiazolyl-C(=N-OR5)-CO-gp (Gp A) , where R5 is vinyl, cyanomethyl or 2-methoxy-2-propyl and R4 is H or a protecting gp or R5 is H, alkyl or a protecting gp and R4 is formyl or trifluoroacetyl; R2 is H, R8-COO-CHR9- (R8 is alkyl or cyclohexyl and R9 is H or alkyl), methoxymethyl, etc and R3 is R'3-SO2-O- or R"3-COO-; R'3 is alkyl, trifluoromethyl, trichloromethyl or phenyl and R"3 is R'3 or acylmethyl,tc or (B) R1 is H or as in (A); R4 is H or a protecting gp and R5 is H, alkyl or a protecting gp), R6 CO-(where R6 is H, alkyl or phenyl), R7-OOC-(where R7 isalkyl nitrophenylthio or R1NH- is replaced by a methyleneimino gp and R2 is as defined in (A) or R1 is H, 1-8C alkanoyl, 2-8C Cl and/or Br substd alkanoyl, azidoacetyl, cyanoacetyl etc. and R2 is 4-6C tert-alkyl, 6-7C tert- alkenyl, 6-7C tert-alkynyl, benzyl etc and R3 is R'3-SO2-O- or R"3-COO, where R'3 is phenyl and R"3 is phenyl, acylmethyl, 2-acylethyl, etc. Unless specifically defined alkyl and acyl gps are 1-4C opt branched gps. When n is 0 (i.e. not the 1- oxide) then the double bond is in position 2- or 3 and when n is 1(the 1-oxide)then the double bond is in position 2-. The 3-group has E. or Z form). (I) are intermediates for 3-thiovinylcephalosporins.</p> |
