【摘要】 <正> 以芬太尼为典型代表物的4-苯胺哌啶类化合物是一类具有独特结构类型、强度高、作用迅速的高效麻醉镇痛剂。该类化合物哌啶环的3位或4位引入适当取代基团能提高镇痛活性,其活性强度已达微克水平。芬太尼类化合物的构效关系研究表明:分子构象与生物活性之间关系密切。虽Peeters和Koch等人分别对芬太尼(R 4263)和4-甲氧甲基芬太尼类代表物(R 30490,R 30730)更多还原

【Abstract】 The crystal structures of methyl 4-[N-（cyclopropyl-carbonyl）-N-phenylamino-]-1（2-phenylethyl）-4-piperidinecarboxylate （R32767） and N-[4-acetyl-1-（2-phenylethyl）-4-piperidinyl]-N-phenylpropanamide （R 32557） have been determined as part of a structure-activity relationship study on a series of 4-substituted fentanyl. R32767: C₂₅H₃₀N₂O₃; triclinic, pl; a=10.280（2）,=b=10.367（1）, c=12.170（1）A, α=92.28（1）, β=102.31（1）, γ=116.83（1）°, Z=2. R32557: C₂₄H₃₀N₂O₂·HCL·2H₂0; triclinic, pl; a=9.369（6）, b=9.680（6）, c=14.799（9）A, α=86.24（5）, β=76.23（5）, γ=68.70（5）°, Z=2. The structures of the two are compared with those of R30490, R30730 and R4263. Preliminary study indicates that its toxicity is concerned with angles between the two aromatic rings and the piperidine ring. The potent analgesic activity may correspond to a torsion angle C₁₄-C₁-N₂-C₁9 （according to locants of R32557） of about 120°.更多还原