Synthesis and muscarinic cholinergic receptor affinities of 3-quinuclidinyl .alpha.-(alkoxyalkyl)-.alpha.-aryl-.alpha.-hydroxyacetates
摘要:
Seven analogues of 3-quinuclidinyl benzilate (QNB) in which one phenyl ring was replaced by an alkoxyalkyl moiety were synthesized and their affinities for the muscarinic cholinergic receptor determined. An oxygen in the beta-position of the moiety was not well-tolerated. By contrast, an oxygen in the gamma-position did not change the affinity for the muscarinic receptor. However, when a bromine was placed on the remaining phenyl ring, the affinity was significantly reduced in striking contrast to results obtained on halogenation of QNB.
Synthesis and muscarinic cholinergic receptor affinities of 3-quinuclidinyl .alpha.-(alkoxyalkyl)-.alpha.-aryl-.alpha.-hydroxyacetates
摘要:
Seven analogues of 3-quinuclidinyl benzilate (QNB) in which one phenyl ring was replaced by an alkoxyalkyl moiety were synthesized and their affinities for the muscarinic cholinergic receptor determined. An oxygen in the beta-position of the moiety was not well-tolerated. By contrast, an oxygen in the gamma-position did not change the affinity for the muscarinic receptor. However, when a bromine was placed on the remaining phenyl ring, the affinity was significantly reduced in striking contrast to results obtained on halogenation of QNB.
A Formal anti-Markovnikov Hydroalkoxylation of Allylic Alcohols with a Ruthenium Catalyst
作者:Yushi Nakamura、Tetsuo Ohta、Yohei Oe
DOI:10.1246/cl.171104
日期:2018.3.5
Hydroalkoxylation of C–C double bonds was achieved through the use of a rutheniumcatalyst. The reaction of allylic alcohols with nucleophilic alcohols was carried out in the presence of a rutheniumcatalyst prepared by RuClH(CO)(PPh3)3 and 2,6-bis(n-butyliminomethyl)-4-(piperidin-1-yl)pyridine under mild reaction conditions to afford the corresponding γ-alkoxypropanols in good yield.
614. Quinolizines. Part II. A synthesis of alkyl- and of aryl-quinolizinium salts
作者:E. E. Glover、Gurnos Jones
DOI:10.1039/jr9580003021
日期:——
Enantioselective chiral borane-mediated aldol reactions of silyl ketene acetals with aldehydes. The novel effect of the trialkysilyl group of the silyl ketene acetal on the reaction course
Highly enantioselective aldol reactions of silyl ketene acetals with a variety of aldehydes were achieved by using chiral boranes prepared from the sulfonamides of alpha-amino acids.
CYCLOPROPANE HYDROCARBONS FROM gamma-BROMOETHERS<sup>1</sup>
作者:J. T. GRAGSON、K. W. GREENLEE、J. M. DERFER、C. E. BOORD
DOI:10.1021/jo01121a001
日期:1955.3
Synthesis of 3-hydroxy aldehydes, 3-hydroxy acetals, and 3-hydroxy ethers from 2-alkoxy oxetanes