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CAS号75-44-5 光气 | CAS号2688-84-8 2-氨基二苯醚 | CAS号2243-42-7 2-苯氧基苯甲酸 | CAS号2770-12-9 N-(2-phenoxyphe... | CAS号119-61-9 二苯甲酮 | CAS号833-50-1 2-苯基苯并恶唑 | CAS号2770-17-4 11-Phenyldibenz... | CAS号2770-15-2 N-(2-phenoxyphe...

📜苯氧苯甲酸置于二苯基膦叠氮化物,三乙胺体系中,用 甲苯 作为反应溶剂,化学反应 0.33H,反应生成 异氰酸2-苯氧基苯酯
参考文献:选择性毒蕈碱拮抗剂.二.联苯基氨基甲酸酯衍生物的合成及其抗毒蕈碱特性.
标题:选择性毒蕈碱拮抗剂.二.联苯基氨基甲酸酯衍生物的合成及其抗毒蕈碱特性.
摘要:合成了一系列新颖的联苯基氨基甲酸酯衍生物,并评估了与m1,M2和m3受体的结合以及抗毒蕈碱活性.受体结合试验表明,联苯-2-基氨基甲酸酯衍生物对m1和m3受体具有高亲和力,对m3受体的选择性高于m2受体,表明联苯-2-基是毒蕈碱中二苯甲基的新型疏水替代物.拮抗剂领域.在这个系列中,奎宁环丁-4-基联苯基-2-基氨基甲酸酯一盐酸盐(8L,Ym-46303)对m1和m3受体的亲和力最高,对m3的选择性高于m2受体.与奥昔布宁相比,Ym-46303在反射性节律性收缩中对膀胱压力的抑制活性约高十倍,对大鼠唾液分泌的膀胱收缩选择性提高约5倍.此外,在体外也观测到选择性拮抗活性.对成年大鼠心动过缓和升压以及小鼠震颤的抗毒蕈碱作用的进一步评估表明,Ym-46303可作为膀胱选择性m3拮抗剂用于尿急性尿失禁的治疗,具有有效的作用和较少的副作用.
DOI:10.1248/cpb.46.1286

专利信息

专利号:US-7138526-B1
优先权日:1999-06-15
标 题 :Solid phase synthesis of n,n-disubstituted diazacycloalkylcarboxy derivatives
发明人：HERPIN TIMOTHY F; MORTON GEORGE C; SALVINO JOSEPH M
权利人:AVENTIS PHARMA INC
摘要:A method for the solid phase synthesis of N,N-disubstituted diazacycloalkylcarboxy derivatives of general formula (I) and (II) is claimed. Examples include piperazine-2-carboxamide. The method is applicable to the synthesis or large combinatorial libraries

专利号:US-6989384-B2
优先权日:2000-06-14
标题:Antipicornaviral compounds and compositions, their pharmaceutical uses, and materials for their synthesis
发明人：HUA YE; LUU HIEP THE; CHAN FORA P; JOHNSON JR THEODORE O; REICH SIEGFRIED HEINZ; SKALITZKY DONALD JAMES; YANG YI; HENDRICKSON THOMAS F; CHU SHAO SONG; EASTMAN BRIAN WALTER
权利人:AGOURON PHARMA
摘要:Compounds of the formula: n nwhere the formula variables are as defined in the disclosure, advantageously inhibit or block the biological activity of the picomaviral 3C protease. These compounds, as well as pharmaceutical compositions containing these compounds, are useful for treating patients or hosts infected with one or more picornaviruses, such as RVP. Intermediates and synthetic methods for preparing such compounds are also described.