| 摘要 |
<p>6-Substd.-methylenepenams of formula (I) and their acid-addn. and n=0, 1 or 2; R1=tetrahydropyranyl, allyl, benzyl, 4-nitro-benzyl, Ph2CH, Cl3CCH2, tBu or phenacyl, as protecting gp.; H; 3-phthalidyl, 4-crotonolactonyl, qamma-butyrolacton-4-yl, CR4R5-OCOR6, CR4R5-O-COOR6, CHR4-OCOR14 or a gp. of formula (II), as an ester gp. readily hydrolysable in vivo; R4, R50H or Me; R6=1-5C alkyl; R14=gp. of formula (III); R15=2-Ph-, 2-PhO-, D-2-amino-2-Ph-, D-2-amino-2-(p-hydroxyphenyl)-, 2-COOH-2-Ph-, 2-COOH-2-(2-thienyl)-, 2-COOH-2-(3-thienyl)- or D-2-(4-ethyl-2,3-dioxopiperazino carbonylamino)-2-Ph-acetoamido or 2,2-dimethyl-4-phenyl--5imidazolidi none-1-yl; one of R2, R3=H; and the other=Cl, CH2OH, vinyl, 1-4C alkylthio, 1-4C alkylsulphonyl, furyl, thienyl, N-methylpyrrolyl, N-acetylpyrrolyl, R7C6H4, R7C6H4S, (a)-(e) X1=S, O or NR11; R7=H, 1-4C alkyl, 1-4C alkoxy, allyloxy, OH, COOH, 2-5C alkoxycarbonyl, (1-5C)alkyl-carbonyl, Ph, PhCH2, naphthyl, pyridyl, NR8R9, CONR8R9, NHCOR10, NO2, Cl Br, CF3 or SR8; R8, R9=H, 1-4C alkyl, Ph or PhCH2.</p> |
