2-乙酰基-3-氧代己酸乙酸置于乙醚,氨体系中,化学反应生成 丁酰乙酸乙酯 参考文献:Differential Effects Of Utp And Atp On Ion Transport In Porcine Tracheal Epithelium 标题:Differential Effects Of Utp And Atp On Ion Transport In Porcine Tracheal Epithelium 摘要:以下是文本的中文翻译: 将猪气管上皮的分离段放置于尤金箱(ussing Chamber)中,监测维持跨上皮电位差为0 Mv所需的电流(短路电流,Isc),并研究核苷酸对isc的影响. 黏膜侧的utp(100 μm)引发短暂的isc上升,随后出现持续30分钟的基线isc下降.黏膜侧的atp(100 μm)同样刺激短暂的isc上升,但与utp不同,它并未抑制基线isc.而基底侧的utp和atp均短暂增加isc. 预刺激utp的上皮对atp无反应,但以atp预刺激并不会消除对utp的反应.这些结果表明,上皮细胞表面存在两组受体,使核苷酸能够调节isc. Utp诱导的上升被预先用布美他尼(100 μm),二苯基氨基-2-羧酸(dpc,1 Mm)或无cl−和hco3−的溶液处理所抑制,而下降则被预先用阿米洛利处理所消除. Thapsigargin(0.3 μm)消除了utp诱导的isc增加,但未影响随后的下降.staurosporine(0.1 μm)抑制基线isc并阻断utp诱导的isc抑制.蛋白激酶c(pkc)抑制剂(d-赤藓醇基鞘氨醇)或蛋白激酶a(pka)抑制剂(h89)均无作用. 本研究表明,Utp刺激cl−分泌并抑制基线na+吸收.atp具有类似的刺激作用,可能是通过激活p2Y2受体和增加[ca2+]In介导,但无抑制作用,这可能是通过激活嘧啶受体并可能抑制其他蛋白激酶(而非pkc或pka). <英国药理学杂志> (2000),130,367-374; Doi:10.1038/sj.Bjp.0703324 DOI:10.1038/sj.Bjp.0703324
专利号:US-2006058532-A1 优先权日:2004-09-10 标 题:Process for the scalable synthesis of 1,3,4,9-tetrahydropyrano[3,4-b]-indole derivatives 发明人:CHEW WARREN; CHEAL GLORIA K; LUNETTA JACQUELINE F; DEMERSON CHRISTOPHER A 权利人:CHEW WARREN; CHEAL GLORIA K; LUNETTA JACQUELINE F; DEMERSON CHRISTOPHER A 摘要:The invention is directed to a process of synthesizing compounds of formula (VI): n n nwherein R 1- R 9 , R 3′ , R 4′ and Y are as set forth in the specification, and said method is useful for large scale synthesis thereof. The invention is also directed to useful intermediates for synthesizing the compounds of formula (VI) and processes of preparing said intermediates.
专利号:US-3950389-A 优先权日:1968-10-04 标 题 :Stereospecific total steroidal synthesis via substituted C/D-trans indanones 发明人:HAJOS ZOLTAN GEORGE 权利人:HOFFMANN LA ROCHE 摘要:Total synthesis of known progestationally active steroidal materials. The steroids can be synthesized depending on the particular starting reactants selected by employing as intermediates bicyclic compounds of the formula ##SPC1## n Wherein m is an integer having a value of 1 or 2; R 4 is hydrogen or lower alkyl; Z is lower alkylenedioxymethylene CH(OR 2 ) and carbonyl; R 8 when taken alone is hydrogen; R 9 when taken alone is lower alkoxycarbonyl, aryloxy-carbonyl, lower cycloalkyloxycarbonyl, carbonyl-halide, hydrogen, carboxy, formyl and methylene-X, where X is a leaving group and when taken together are methylene; with the proviso that when Z is carbonyl R 8 when taken alone is hydrogen; R 9 when taken alone is carbonyl halide, hydrogen, carboxy, formyl and methylene-X where X is a leaving group and when taken together are methylene and R 2 is hydrogen, lower alkyl, lower alkoxy-lower alkyl, phenyl-lower alkyl, tetrahydropyranyl, lower alkanoyl, benzoyl, nitrobenzoyl, carboxy-lower alkanoyl, carboxybenzoyl, trifluoroacetyl and camphorsulfonyl n And reacting them in the case where R 8 and R 9 taken together are methylene or R 8 is hydrogen and R 9 is methylene-X with β-keto esters and other analogs of the formula ##EQU1## wherein R.sub. 6 is selected from the group CONSISTING OF ##EQU2## and LOWER ALKYL; R 7 is lower alkyl; R 15 is selected from the group consisting of oxo, lower alkylene-dioxy or (hydrogen and lower alkoxy); B is selected from the group consisting of lower alkoxy-carbonyl-methylene, lower-aryloxy-carbonyl-methylene, cyanomethylene, lower alkyl sulfinyl-methylene, lower alkyl sulfonyl-methylene, and R 25 and R 26 are independently selected from the group consisting of hydrogen, hydroxyl and lower alkyl.
专利号:US-4077983-A 优先权日:1974-06-24 标 题:Stereospecific total steroidal synthesis via substituted C/D-trans indanones 发明人:HAJOS ZOLTAN GEORGE 权利人:HOFFMANN LA ROCHE 摘要:Total synthesis of known progestationally active steroidal materials. The steroids can be synthesized depending on the particular starting reactants selected by employing as intermediates bicyclic compounds of the formula ##STR1## wherein m is an integer having a value of 1 or 2; R 4 is hydrogen or lower alkyl; Z is lower alkylenedioxy, CH(OR 2 ) and carbonyl; R 8 when taken alone is hydrogen; R 9 when taken alone is lower alkoxycarbonyl, aryloxy-carbonyl, lower cycloalkyloxycarbonyl, carbonyl-halide, hydrogen, carboxy, formyl and methylene-X, where X is a leaving group and when taken together are methylene; with the proviso that when Z is carbonyl R 8 when taken alone is hydrogen; R 9 when taken alone is carbonyl halide, hydrogen, carboxy, formyl and methylene-X where X is a leaving group and when taken together are methylene and R 2 is hydrogen, lower alkyl, lower alkoxy-lower alkyl, phenyl-lower alkyl, tetrahydropyranyl, lower alkanoyl, benzoyl, nitrobenzoyl, carboxy-lower alkanoyl, carboxybenzoyl, trifluoroacetyl and camphorsulfonyl n And reacting then in the case where R 8 and R 9 taken together are methylene or R 8 is hydrogen and R 9 is methylene-X with β-keto esters and other analogs of the formula ##STR2## wherein R 6 is selected from the group consisting of ##STR3## lower alkyl; R 7 is lower alkyl; R 15 is selected from the group consisting of oxo, lower alkylenedioxy or (hydrogen and lower alkoxy); B is selected from the group consisting of lower alkoxy-carbonylmethylene, lower-aryloxy-carbonyl-methylene, cyanomethylene, lower alkyl sulfinyl-methylene, lower alkyl sulfonyl-methylene, and R 25 and R 26 are independently selected from the group consisting of hydrogen, hydroxyl and lower alkyl.
专利号:US-3984473-A 优先权日:1968-10-04 标题 :Stereospecific total steroidal synthesis via substituted C/D-trans indanones 发明人:HAJOS ZOLTAN GEORGE 权利人:HOFFMANN LA ROCHE 摘要:Total synthesis of known progestationally active steroidal materials. The steroids can be synthesized depending on the particular starting reactants selected by employing as intermediates bicyclic compounds of the formula ##SPC1## n Wherein m is an integer having a value of 1 or 2; R 4 is hydrogen or lower alkyl; Z is lower alkylenedioxy, CH(OR 2 ) and carbonyl; R 8 when taken alone is hydrogen; R 9 when taken alone is lower alkoxy-carbonyl, aryloxy-carbonyl, lower cycloalkyloxy-carbonyl, carbonyl-halide, hydrogen, carboxy, formyl and methylene-X, where X is a leaving group and when taken together are methylene; with the proviso that when Z is carbonyl R 8 when taken alone is hydrogen; R 9 when taken alone is carbonyl halide, hydrogen, carboxy, formyl and methylene-X where X is a leaving group and when taken together are methylene and R 2 is hydrogen, lower alkyl, lower alkoxy-lower alkyl, phenyl-lower alkyl, tetrahydropyranyl, lower alkanoyl, benzoyl, nitrobenzoyl, carboxy-lower alkanoyl, carboxy-benzoyl, trifluoroacetyl and camphorsulfonyl and reacting them in the case where R 8 and R 9 taken together are methylene or R 8 is hydrogen and R 9 is methylene-X with β-keto esters and other analogs of the formula ##EQU1## wherein R 6 is selected from the group consisting of ##EQU2## and lower alkyl; R 7 is lower alkyl; R 15 is selected from the group consisting of oxo, lower alkylene-dioxy or (hydrogen and lower alkoxy); B is selected from the group consisting of lower alkoxy-carbonyl-methylene, lower-aryloxy-carbonyl-methylene, cyanomethylene, lower alkyl sulfinyl-methylene, lower alkyl sulfonyl-methylene, and R 25 and R 26 are independently selected from the group consisting of hydrogen, hydroxyl and lower alkyl.
专利号:US-3985733-A 优先权日:1968-10-04 标题 :Stereospecific total steroidal synthesis via substituted C/D-trans indanones 发明人:HAJOS ZOLTAN GEORGE 权利人:HOFFMANN LA ROCHE 摘要:Total synthesis of known progestationally active steroidal materials. The steroids can be synthesized depending on the particular starting reactants selected by employing as intermediates bicyclic compounds of the formula ##SPC1## n Wherein m is an integer having a value of 1 or 2; R 4 is hydrogen or lower alkyl; Z is lower alkylenedioxy, CH(OR 2 ) and carbonyl; R 8 when taken alone is hydrogen; R 9 when taken alone is lower alkoxy-carbonyl, aryloxy-carbonyl, lower cycloalkyloxy-carbonyl, carbonyl-halide, hydrogen, carboxy, formyl and methylene-X, where X is a leaving group and when taken together are methylene; with the proviso that when Z is carbonyl R 8 when taken alone is hydrogen; R 9 when taken alone is carbonyl halide, hydrogen, carboxy, formyl and methylene-X where X is a leaving group and when taken together are methylene and R 2 is hydrogen, lower alkyl, lower alkoxy-lower alkyl, phenyl-lower alkyl, tetrahydropyranyl, lower alkanoyl, benzoyl, nitrobenzoyl, carboxy-lower alkanoyl, carboxy-benzoyl, trifluoroacetyl and camphorsulfonyl n And reacting them in the case where R 8 and R 9 taken together are methylene or R 8 is hydrogen and R 9 is methylene-X with β-keto esters and other analogs of the formula ##EQU1## wherein R 6 is selected from the group CONSISTING OF ##EQU2## and LOWER ALKYL; R 7 is lower alkyl; R 15 is selected from the group consisting of oxo, lower alkylenedioxy or (hydrogen and lower alkoxy); B is selected from the group consisting of lower alkoxy-carbonyl-methylene, lower-aryloxy-carbonyl-methylene, cyanomethylene, lower alkyl sulfinyl-methylene, lower alkyl sulfonyl-methylene, and R 25 and R 26 are independently selected from the group consisting of hydrogen, hydroxyl and lower alkyl.
专利号:US-4052413-A 优先权日:1974-06-24 标 题:Stereospecific total steroidal synthesis via substituted c/d-trans indanones 发明人:HAJOS ZOLTAN GEORGE 权利人:HOFFMANN LA ROCHE 摘要:Total synthesis of known progestationally active steroidal materials. The steroids can be synthesized depending on the particular starting reactants selected by employing as intermediates bicyclic compounds of the formula ##STR1## WHEREIN M IS AN INTEGER HAVING A VALUE OF 1 OR 2; R 4 is hydrogen or lower alkyl; Z is lower alkylenedioxy, CH(OR 2 ) and carbonyl; R 8 when taken alone is hydrogen; R 9 when taken alone is lower alkoxycarbonyl, aryloxy-carbonyl, lower cycloalkyloxycarbonyl, carbonyl-halide, hydrogen, carboxy, formyl and methylene-X, where X is a leaving group and when taken together are methylene; with the proviso that when Z is carbonyl R 8 when taken alone is hydrogen; R 9 when taken alone is carbonyl halide, hydrogen, carboxy, formyl and methylene-X where X is a leaving group and when taken together are methylene and R 2 is hydrogen, lower alkyl, lower alkoxy-lower alkyl, phenyl-lower alkyl, tetrahydropyranyl, lower alkanoyl, benzoyl, nitrobenzoyl, carboxy-lower alkanoyl, carboxy-benzoyl, trifluoroacetyl and camphorsulfonyl n And reacting them in the case where R 8 and R 9 taken together are methylene or R 8 is hydrogen and R 9 is methylene-X with β-keto esters and other analogs of the formula ##STR2## wherein R 6 is selected from the group consisting of ##STR3## and lower alkyl; R 7 is lower alkyl; R 15 is selected from the group consisting of oxo, lower alkylenedioxy or (hydrogen and lower alkoxy); B is selected from the group consisting of lower alkoxy-carbonyl-methylene, lower-aryloxy-carbonyl-methylene, cyanomethylene, lower alkyl sulfinyl-methylene, lower alkyl sulfonyl-methylene, and R 25 and R 26 are independently selected from the group consisting of hydrogen, hydroxyl and lower alkyl.