| 摘要 |
<p>Prepn. of azetidinone derivs. of formula (I) or their salts or readily cleavable esters is carried out by (a) reacting an azetidinone deriv. of formula (II), or a readily cleavable ester of (II), with a silylated vinyl cpd. of formula R4R5C=CZ-X-Si(R11)3 (III), or a readily cleavable ester of (III); (b) hydrolysing the reaction mixt.; and opt. (c) cleaving ester prods. and/or esterifying free acids or converting them to salts with a base. In the formulae, A is H or (CH2CX)nYR2; X and Y are O or S; R1 is H, 1-4C alkyl, CH2COOR6, C(COOR6):P(R7)3, C(COOR6):C(Me)2 or an amino-protecting gp.; R2 and R6 are H or 1-6C alkyl; R3 is H, NHR8 or phthalimido; R4 is H, 1-6C alkyl or Ar; R5 is H, 1-6C alkyl or 2-7C alkoxycarbonyl; R7 is Ph or n-Bu; R8 is COCH2R9 or C(Ph)3; R9 is H, 1-16C alkyl, Ar or ArO; Ar is phenyl opt. substd. by F, Cl, Br, I, NO2, OH, 1-4C alkyl . or 1-4C alkoxy; n is 0 or 1; E is Cl, Br or OCOR10; R10 is 1-17C alkyl or Ar; each R11 is independently 1-4C alkyl. The use of (I), which are mostly new, in the synthesis of beta-lactamase inhibiting and/or antibacterial beta-lactam is claimed.</p> |
