CAS: 25026-34-0; 2-(4-Chlorophenyl)Acetyl Chloride

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CAS号1878-66-6 4-氯苯乙酸 | CAS号79-37-8 草酰氯 | CAS号3282-33-5 Ethanone,1-(4-c... | CAS号122-01-0 4-氯苯甲酰氯 | CAS号74-11-3 对氯苯甲酸 | CAS号873-76-7 4-氯苄醇 | CAS号622-95-7 4-氯溴苄 | CAS号140-53-4 对氯苯乙腈 | CAS号104-03-0 对硝基苯乙酸 | CAS号104941-08-4 2-(4-chlorophen... | CAS号5586-88-9 4-氯苯丙酮 | CAS号57676-51-4 4-氯苯乙酰肼 | CAS号5468-97-3 1-(4-氯苯基)-2-甲基-2-丙醇 | CAS号14310-22-6 1-chloro-4-(2-p... | CAS号938-95-4 4-(氯甲基)苯乙酸 | CAS号3457-46-3 4,4'-二氯苯偶酰 | CAS号232267-03-7 1-(4-chlorophen... | CAS号22711-23-5 对氯联苯酰 | CAS号1878-66-6 4-氯苯乙酸

对氯苯乙酸置于草酰氯体系中,用 氯仿 用作溶剂,化学反应生成对氯苯乙酰氯
参考文献:(2S)-1-(芳基乙酰基)-2-(氨基甲基)哌啶衍生物:新颖的高选择性κ阿片类镇痛药.
标题:(2S)-1-(芳基乙酰基)-2-(氨基甲基)哌啶衍生物:新颖的高选择性κ阿片类镇痛药.
摘要:本文描述了新型的1-(芳基乙酰基)-2-(氨基甲基)哌啶衍生物的合成和构效关系,作为κ阿片类镇痛药.通过计算研究和1H NMR定义了具有60度扭转角(n1C2C7N8)的药效团的活性构象.芳香族部分取代的定量结构-活性关系研究表明,对位和/或间位存在吸电子和亲脂性取代基是非常好的镇痛活性和κ亲和力所必需的.铅化合物(2S)-1-[((3,4-二氯苯基)乙酰基]-2-(吡咯烷-1-基甲基)哌啶盐酸盐和(2S)-1-[4-(三氟甲基)苯基]乙酰基]-2-(吡咯烷-1-基甲基)哌啶盐酸盐的kappa / Mu选择性最高(分别为6500:1和4100:1)以及迄今为止鉴定出的最有力的(κκ0.24和0.57 Nm)κ配体.在抗伤害感受的小鼠甩尾模型中,化合物14(ed50 = 0.05 Mg / Kg Sc)的效力是吗啡的25倍,效力是标准kappa配体u-50488的16倍.
Doi:10.1021/jm00105A061

专利信息

专利号:US-10865390-B2
优先权日:2018-02-12
标 题 :Alcohol dehydrogenase mutant and application thereof in synthesis of diaryl chiral alcohols
发明人：NI YE; ZHOU JIEYU; XU GUOCHAO; WANG YUE
权利人:UNIV JIANGNAN
摘要:The present disclosure discloses an alcohol dehydrogenase mutant and application thereof in synthesis of diaryl chiral alcohols, and belongs to the technical field of bioengineering. The alcohol dehydrogenase mutant of the present disclosure has excellent catalytic activity and stereoselectivity, and may efficiently catalyze the preparation of a series of chiral diaryl alcohols in R- and S-configurations. By coupling alcohol dehydrogenase of the present disclosure to glucose dehydrogenase or formate dehydrogenase, the synthesis of chiral diaryl alcohol intermediates of various antihistamines may be achieved. Compared with the prior art, a method for preparing diaryl chiral alcohols through asymmetric catalytic reduction using the alcohol dehydrogenase of the present disclosure has the advantages of simple and convenient operation, high substrate concentration, complete reaction and high product purity, and has great industrial application prospects.

专利号:US-7098354-B2
优先权日:2002-10-25
标 题:Racemoselective synthesis of rac-diorganosilylbis(2-methylbenzo[e]indeyl)zirconium compounds
发明人：DAMRAU HANS-ROBERT; MUELLER PATRIK; GARCIA VALERIE; SIDOT CHRISTIAN; TELLIER CHRISTIAN; LELONG JEAN-FRANCOIS
权利人:BASELL POLYOLEFINE GMBH
摘要:The present invention relates to a specific process for the diastereoselective synthesis of rac-diorganosilylbis(2-methylbenzo[e]indenyl)zirconium compounds of the formula I, n nby reacting the silyl-bridged bisindenyl ligand with a dihalozirconium bis(3,5-di-tert-butylphenoxide)-base adduct to form the diorganosilylbis(2-methylbenzo[e]indenyl)zirconium bis(3,5-di-tert-butylphenoxide) and subsequently replacing the phenoxide groups by X using suitable replacement reagents to give the compound of the formula I; where the substituents X can be identical or different and are each F, Cl, Br, I or linear, cyclic or branched C 1-10 -alkyl; and the substituents R can be identical or different and are each linear, cyclic or branched C 1-10 -alkyl or C 6-10 -aryl; and also to the use of these compounds as catalysts.

专利号:US-6608196-B2
优先权日:2001-05-03
标题 :Process for solid supported synthesis of pyruvate-derived compounds
发明人：WANG BING; JANAGANI SATYANARAYANA; CALLAWAY WYETH B; SESSLER JONATHAN L
权利人:GALILEO PHARMACEUTICALS INC
摘要:Provided are processes for synthesizing structurally diverse pyruvate-derived compounds using a parallel approach on a solid phase support. Examples of such a solid phase support include resins which have also been used in solid phase peptide synthesis.

专利号:US-6413957-B1
优先权日:1998-04-21
标题:Methods of inhibiting cell proliferation using indeno [1,2-c]pyrazol-4-ones
发明人：NUGIEL DAVID A; CARINI DAVID J; DI MEO SUSAN V; YUE EDDY W
权利人:BRISTOL MYERS SUIBB PHARMA COM
摘要:The present invention relates to the synthesis of a new class of indeno[1,2-c]pyrazol-4-ones of formula (I): n that are potent inhibitors of the class of enzymes known as cyclin dependent kinases, which relate to the catalytic subunits cdk1-7 and their regulatory subunits know as cyclins A-G. This invention also provides a novel method of treating cancer or other proliferative diseases by administering a therapeutically effective amount of one of these compounds or a pharmaceutically acceptable salt form thereof. Alternatively, one can treat cancer or other proliferative diseases by administering a therapeutically effective combination of one of the compounds of the present invention and one or more other known anti-cancer or anti-proliferative agents.

专利号:US-8129560-B2
优先权日:2005-08-15
标 题 :Process for the synthesis of mandipropamid and derivatives thereof
发明人：BOWDEN MARTIN CHARLES; CLARK THOMAS AITCHESON; GIORDANO FANNY; JAU BEAT; SCHNEIDER HANS-DIETER; SEIFERT GOTTFRIED; ZELLER MARTIN; FABER DOMINIK; WISS JUERG
权利人:BOWDEN MARTIN CHARLES; CLARK THOMAS AITCHESON; GIORDANO FANNY; JAU BEAT; SCHNEIDER HANS-DIETER; SEIFERT GOTTFRIED; ZELLER MARTIN; FABER DOMINIK; WISS JUERG; SYNGENTA CROP PROT INC
摘要:A process for the preparation of a compound of formula (I), the process comprising: (i) the reaction of a compound of formula (III), with a compound of formula (IV) to give a compound of formula (II), and (ii) the reaction of the compound of formula (II) with a leaving group, to give the compound of formula (I).

专利号:US-7250435-B2
优先权日:1999-10-20
标 题:Acylsemicarbazides as cyclin dependent kinase inhibitors useful as anti-cancer and anti-proliferative agents
发明人：NUGIEL DAVID A; CARINI DAVID J; DI MEO SUSAN V; VIDWANS ANUP P; YUE EDDY
权利人:BRISTOL MYERS SQUIBB PHARMA CO
摘要:The present invention relates to the synthesis of a new class of indeno[1,2-c]pyrazol-4-ones of formula (I): n nthat are potent inhibitors of the class of enzymes known as cyclin dependent kinases, which relate to the catalytic subunits cdk1-7 and their regulatory subunits know as cyclins A-G.n n This invention also provides a novel method of treating cancer or other proliferative diseases by administering a therapeutically effective amount of one of these compounds or a pharmaceutically acceptable salt form thereof. Alternatively, one can treat cancer or other proliferative diseases by administering a therapeutically effective combination of one of the compounds of the present invention and one or more other known anti-cancer or anti-proliferative agents.