[EN] A PROCESS FOR THE SYNTHESIS OF ANTHRANILIC ACID/AMIDE COMPOUNDS AND INTERMEDIATES THEREOF [FR] PROCÉDÉ DE SYNTHÈSE DE COMPOSÉS ACIDE ANTHRANILIQUE/AMIDE ET INTERMÉDIAIRES DE CEUX-CI
[EN] ENHANCED NEOGLYCOSIDES THROUGH NEOGLYCOSYLATION AND METHODS OF USE THEREOF<br/>[FR] NÉO-GLYCOSIDES AMÉLIORÉS PAR NÉO-GLYCOSYLATION ET LEURS PROCÉDÉS D'UTILISATION
申请人:WISCONSIN ALUMNI RES FOUND
公开号:WO2010080863A1
公开(公告)日:2010-07-15
Using neoglycosylation, the impact of differential glycosylation upon the divergent anticancer and anti-HIV properties of the triterpenoid betulinic acid (BA) was examined. Each member from a library of 37 differentially glycosylated BA variants was tested for anticancer and anti-HIV activities. Enhanced analogs for both desired activities were discovered with the corresponding antitumor or antiviral enhancements diverging, based upon the appended sugar, into two distinct compound subsets.
Palladium(II)-Catalyzed Directed <i>anti-</i>Hydrochlorination of Unactivated Alkynes with HCl
作者:Joseph Derosa、Annabelle L. Cantu、Mark N. Boulous、Miriam L. O’Duill、Joshua L. Turnbull、Zhen Liu、Daizy M. De La Torre、Keary M. Engle
DOI:10.1021/jacs.7b00892
日期:2017.4.12
A regioselective anti-hydrochlorination of unactivated alkynes is reported. The reaction utilizes in situ generated HCl as the source of both the Cl- and H+ and is catalyzed by palladium(II) acetate, with loadings as low as 25 ppm. Removable picolinamide and 8-aminoquinoline bidentate directing groups are used to control the regioselectivity of the chloropalladation step and stabilize the resulting
报道了未活化炔烃的区域选择性抗氢氯化作用。该反应利用原位生成的 HCl 作为 Cl- 和 H+ 的来源,并由乙酸钯 (II) 催化,负载量低至 25 ppm。可去除的吡啶甲酰胺和 8-氨基喹啉二齿导向基团用于控制氯钯化步骤的区域选择性,并稳定所得的链烯基钯 (II) 中间体,用于随后的原脱钯反应。该方法提供了以优异的产率和高区域选择性获得广泛的取代链烯基氯的途径。这种转化的产物通过 Stille 偶联成功衍生为多种三取代烯烃产物。进行了反应进程动力学分析,揭示了该催化过程的可能机制。
Synthesis of substituted isatins
作者:Larry L. Klein、Michael D. Tufano
DOI:10.1016/j.tetlet.2012.12.035
日期:2013.2
Isatins are valuable intermediates for heterocyclic chemistry. Most of the common methods for their production are less than adequate when the number and lipophilicity of substituents on the targeted isatin are increased. Our group desired such molecules and identified an alternative method for their production.
Palladium-Catalyzed Direct Functionalization of 2-Aminobutanoic Acid Derivatives: Application of a Convenient and Versatile Auxiliary
作者:Mengyang Fan、Dawei Ma
DOI:10.1002/anie.201306583
日期:2013.11.11
New group on the block: 2‐Methoxyiminoacetyl is a readily available auxiliary for promoting palladium‐catalyzed γ arylation of C(sp3)H bonds. This auxiliary can be easily removed by either treatment with 1 n KOH at room temperature, or converted into a glycine moiety for peptide synthesis.
上一个新的基团:2-甲氧基亚氨基乙酰基是促进钯催化C(sp 3)H键的γ芳基化的现成辅助剂。通过在室温下用1 n KOH处理,可以轻松除去该助剂,也可以将其 转化为用于肽合成的甘氨酸部分。
[EN] N-SUBSTITUTED IMINO HETEROCYCLIC COMPOUNDS<br/>[FR] COMPOSÉS HÉTÉROCYCLIQUES DE TYPE IMINO N-SUBSTITUÉS
申请人:BASF SE
公开号:WO2015091649A1
公开(公告)日:2015-06-25
The present invention relates to N-substituted imino compound of formula (I), wherein Y is a radical Y1, Y2, Y3, Y4 or Y5, where Y1 is O-C(=X)-R3; Y2 is S-C(=X)-R3; Y3 is N(R5)-C(=X)-R3; Y4 is N(R5)-S(=O)-R4; Y5 is N(R5)-S(=O)2-R4; and where X is O or S; Het is a 5 or 6 membered carbon-bound or nitrogen-bound heterocyclic ring, W1-W2-W3-W4 represents a carbon chain group connected to N and C=N, and thus forming a saturated, unsaturated, or partially unsaturated 5 or 6 membered nitrogen containing heterocycle, wherein W1, W2, W3 and W4 each individually represent CRVRW; R1, R2 may be hydrogen, halogen, C1-C6-alkyl etc.; and where R3, R4 and R5 are as defined herein. The invention also relates to the use of the N-acylimino heterocyclic compounds, their stereoisomers, their tautomers and their salts, for combating invertebrate pests. Furthermore the invention relates also to methods of combating invertebrate pests, which comprises applying such compounds.