Asymmetric ortho-lithiation of 1,n-dioxa[n]paracyclophane derivatives for the generation of planar chirality
摘要:
The asymmetric induction of planar chirality in 1,n-dioxa[n]paracyclophane derivatives via asymmetric ortho-lithiation is described. Enantioselective ortho-lithiation of unflippable 1,n-dioxa[n]paracyclophanes (n <= 11) using sec-BuLi-(-)-sparteine at -78 degrees C and subsequent treatment with electrophiles gave the corresponding planar-chiral monosubstituted paracyclophanes with excellent ee. Further lithiation of these compounds and treatment with electrophiles gave planar-chiral paracyclophanes with two different substituents. Dilithiation of unflippable 1,n-dioxa[n]paracyclophanes gave the corresponding C(2)symmetrical disubstituted products with almost perfect ee. In the case of flippable 1,n-dioxa[n]paracyclophanes (n >= 12), a stepwise reaction was required for the highly enantioselective formation of disubstituted products. (C) 2011 Elsevier Ltd. All rights reserved.
Monophosphine and diphosphine ligands for diplatinum polyynediyl complexes: Efficient syntheses of new functionality-containing systems and model compounds
作者:Laura de Quadras、Jürgen Stahl、Fedor Zhuravlev、John A. Gladysz
DOI:10.1016/j.jorganchem.2006.12.023
日期:2007.4
similarly yield R2P(CH2)mPR2 (m/R = 8/a, 95%; 14/a, 96%; 14/p-C6H4-t-Bu, 98%). Reactions of KPPh2 with Br(CH2)m′CHCH2and Br(CH2)7CH3 give the corresponding monophosphines Ph2P(CH2)m′CHCH2 (m′ = 7, 82%; 10, 84%) and Ph2P(CH2)7CH3 (85%). When the former is combined with [Pt(μ-Cl)(C6F5)(tht)]2 (tht = tetrahydrothiophene), trans-(C6F5)(Ph2P(CH2)m′CHCH2)2PtCl (77–70%) is isolated. When the latter (excess)
A Photoirradiative Phase-Vanishing Method: Efficient Generation of HBr from Alkanes and Molecular Bromine and Its Use for Subsequent Radical Addition to Terminal Alkenes
phase-vanishing (PV) system comprised of an alkane, perfluorohexanes, and bromine was successfully combined by photoirradiation to efficiently generate hydrogenbromide, which underwent radicaladdition with 1-alkenes in the hydrocarbon layer to afford terminal bromides in high yields.
[EN] LIPOPHOSPHONOXINS, THEIR PREPARATION AND USE<br/>[FR] LIPOPHOSPHONOXINES, LEUR PRÉPARATION ET LEUR UTILISATION
申请人:USTAV ORGANICKE CHEMIE A BIOCHEMIE AV CR V V I
公开号:WO2021115503A1
公开(公告)日:2021-06-17
Described herein are lipophosphonoxins of general formula I, diastereomers and mixtures of diastereomers of compounds of general formula I and their pharmaceutically acceptable salts and hydrates as antibacterial agents, forming an active ingredient in pharmaceutical compositions for the treatment of resistant bacterial infections, disinfectants and/or selective culture media.
.beta.1-Selective adrenoceptor antagonists. 1. Synthesis and .beta.-adrenergic blocking activity of a series of binary (aryloxy)propanolamines
作者:R. W. Kierstead、A. Faraone、F. Mennona、J. Mullin、R. W. Guthrie、H. Crowley、B. Simko、L. C. Blaber
DOI:10.1021/jm00365a004
日期:1983.11
A series of binary (aryloxy)propanolamines has been prepared and examined in vitro and in vivo for beta-adrenoreceptor blockingactivity. These symmetrical compounds consist of two (S)-(phenyloxy)propanolamine pharmacophores coupled through alkylenedioxy or poly(oxyethylenedioxy) linking units of varying lengths. Examples of such binary compounds linked through the 2,2', 3,3', and 4,4' positions in
[EN] DEUTERATED TETRAMETHYL DIOIC ACIDS, COMPOSITIONS COMPRISING THEM AND USES THEREOF<br/>[FR] ACIDES DIOÏQUES DE TÉTRAMÉTHYLE DEUTÉRÉS, COMPOSITIONS LES COMPRENANT ET LEURS UTILISATIONS
申请人:SYNDROMEX LTD
公开号:WO2013084237A1
公开(公告)日:2013-06-13
This invention relates to deuterated tetramethyl dioic acids, compositions comprising them and uses thereof in the treatment of Metabolic Syndrome and any diseases, disorders or symptoms associated therewith.