Allosteric Modulators of the Tertiary Alkanebisamino-Type. Variation of the Substitution of the Middle Chain Nitrogens
摘要:
Synthesis pathways of high flexibility for variously substituted alkanebisamine-type allosteric modulators of musearinic receptors capable of passing the blood-brain barrier were developed starting either from N,N'-(hexane-1,6-diyl)bistosylamide or adipic acid chloride. Pharmacological evaluation of some representative compounds revealed the allosteric potency to fall in a submicromolar range.
Further studies in the acyl-type radical additions promoted by SmI 2 : mechanistic implications and stereoselective reduction of the keto-functionality
摘要:
Attempts were made to promote the carbonyl coupling of cyclohexanone to 4-pyridylthioesters of N-carbamate-protected amino acids with the one electron reducing agent, samarium diiodide. Such reactions proved unsuccessful due to the inability of the ketyl-type radical anion intermediate to be reduced to the corresponding dianion at -78degreesC. Nevertheless, these results explain our recently published work on the high efficiency of the SmI2-mediated acyl-type radical additions of the same thioesters with electron deficient alkenes [J. Am. Chem. Soc. 2003, 125, 4030]. A study was also undertaken to examine methods for the stereoselective reduction of N-carbamate-protected amino ketones to either the syn- or anti-vicinal amino alcohols. In most cases, LiAl(0-t-Bu)(3)H and (S)-Alpine-Hydride were found to effectively provide the anti- and syn-amino alcohols, respectively. The SmI2-promoted reduction of the same ketones afforded a majority of the syn-isomer with selectivities of approximately 5:1. However, in one case, the SmI2-promoted reduction was found to be more effective than that of (S)-Alpine-Hydride. (C) 2003 Elsevier Ltd. All rights reserved.
Beyond the Five and Six: Evaluation of Seven-Membered Cyclic Anhydrides in the Castagnoli–Cushman Reaction
作者:Mykhailo I. Adamovskyi、Sergey V. Ryabukhin、Dmitriy A. Sibgatulin、Eduard Rusanov、Oleksandr O. Grygorenko
DOI:10.1021/acs.orglett.6b03426
日期:2017.1.6
method worked with imines generated from aromatic or α-branched aliphatic aldehydes and is amenable for both parallel synthesis and scale-up. The procedure for epimerization of the resulting trans-disubstituted tetrahydrobenzo[d]azepines to their cis isomers was also developed.
与苯并[ d ]氧杂环庚烷-2,4(1 H,5 H)-二酮作为酸酐组分的Castagnoli–Cushman反应可用于制备2,3-二取代的4-氧代-2,3,4,5-四氢呋喃-1 H-苯并[ d ]氮杂-1-羧酸的产率为21–75%,反式非对映选择性良好。该方法适用于由芳族或α-支化脂族醛生成的亚胺,适用于平行合成和放大。还开发了将所得的反式-二取代的四氢苯并[ d ]氮杂环庚烷异构化成其顺式异构体的方法。
Cleavage of 1,3-dicarbonyls through oxidative amidation
作者:Phillip Biallas、Andreas P. Häring、Stefan F. Kirsch
DOI:10.1039/c7ob00731k
日期:——
A mild and convenient protocol for the oxidative cleavage of 1,3-diketone compounds is described. Under metal-free conditions, the method converts the 1,3-dicarbonyls into amides when treated with (nBu4N)N3 and iodine in the presence of an amine at room temperature. Using this method, a range of 1,3-dicarbonyls with various structural motifs including sterically demanding substituents and ordinary
描述了一种温和方便的方案,用于1,3-二酮化合物的氧化裂解。在无金属的条件下,该方法在室温下在胺的存在下用(n Bu 4 N)N 3和碘处理时,可将1,3-二羰基化合物转化为酰胺。使用这种方法,很容易将一系列具有各种结构基序的1,3-二羰基(包括空间上必不可少的取代基和普通官能团)片段化,并证明环状的1,3-二羰基可以通过开环直接转化为无环二酰胺。 。最初的机理研究表明,烯醇形式的叠氮化后是胺的亲核取代。
POLYESTERS WITH LOW MOLECULAR WEIGHT ADDITIVES FOR IMPROVED GAS BARRIER PROPERTIES
申请人:Peters Richard Dalton
公开号:US20120199515A1
公开(公告)日:2012-08-09
Disclosed is a polyester polymer composition comprising at least one polyethylene terephthalate polyester in an amount ranging from 94.0 weight percent to 99.5 weight percent and at least one additive in an amount ranging from 0.5 weight percent to 6 weight percent, each based on the total weight of the polyester composition. The at least one additive comprises a diamide molecule. The composition of the present invention is useful in producing shaped articles such as, for example, sheeting, films, tubes, bottles, preforms, and profiles. These articles can exhibit improved gas barrier properties. The process for making the polymer composition and the shaped articles is also disclosed.
An oxygen absorber is provided that contains at least one of compounds each having a particular structure, and the oxygen absorber exhibits an oxygen absorbing capability without a metal contained, and is suitable for removing oxygen inside a packaging material packaging foods or the like.
Disclosed herein are articles comprising polymer compositions that can provide a barrier to carbon dioxide diffusion. The disclosed polymer compositions can be utilized in packaging to retard or prevent the diffusion of carbon dioxide out of a carbonated liquid, inter alia, a carbonated soft drink. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.