- Visible light photoredox catalyzed deprotection of 1,3-oxathiolanes
-
An efficient visible light photoredox catalyzed aerobic deprotection of 1,3-oxathiolanes using organic dye Eosin Y as a photocatalyst is disclosed. The deprotection procedure features the use of a metal-free catalyst, mild conditions, a broad range of substrate scope, and good functional group tolerance. 35 examples were tested under the standard conditions and most of them afforded the deprotected products in modest to high yields.
- Yang, Mingyang,Xing, Zhimin,Fang, Bowen,Xie, Xingang,She, Xuegong
-
supporting information
p. 288 - 291
(2020/01/13)
-
- Synthesis of cyclic selenenate/seleninate esters stabilized by ortho-nitro coordination: Their glutathione peroxidase-like activities
-
The syntheses of selenenate/seleninate esters and related derivatives by aromatic nucleophilic substitution (SNAr) reactions of 2-bromo-3-nitrobenzylalcohol (13) and 2-bromo-3-nitrobenzaldehyde (17) with Na2Se2/nBuSeNa are
- Singh, Vijay P.,Singh, Harkesh B.,Butcher, Ray J.
-
p. 1431 - 1442
(2013/01/11)
-
- Synthesis, biological assessment and molecular modeling of new dihydroquinoline-3-carboxamides and dihydroquinoline-3-carbohydrazide derivatives as cholinesterase inhibitors, and Ca channel antagonists
-
The synthesis, biological evaluation, and molecular modeling of new 4-hydroxy-2-oxo-1,2-dihydroquinoline-3-carboxamides(4), 4-hydroxy-2-oxo-1,2- dihydroquinoline-3-carbohydrazide (6), and some hexahydropyrimido[5,4-c] quinoline-2,5-diones (9) produced earlier by our laboratory, as AChE/BuChE inhibitors, is described. From these analyses compound 4c resulted equipotent regarding the inhibition of cholinesterases'; inhibitors 6k, 9a, 9b were selective for AChE, whereas product 4d proved selective for BuChE. Docking analysis has been carry out in order to identify the binding mode in the active site, and to explain the observed selectivities. Only compound 9a has been shown to decrease K+-induced calcium signals in bovine chromaffin cells.
- Tomassoli, Isabelle,Ismaili, Lhassane,Pudlo, Marc,De Los Ríos, Cristóbal,Soriano, Elena,Colmena, Inés,Gandía, Luis,Rivas, Luis,Samadi, Abdelouahid,Marco-Contelles, José,Refouvelet, Bernard
-
experimental part
p. 1 - 10
(2011/02/27)
-
- Preparation and NMR analysis of 2,6-heterodifunctional halobenzenes as precursors for substituted biphenyls
-
Preparation and complete characterization of 16 2,6-disubstituted halobenzenes, including nine new compounds, from two common starting materials is described. Seven of the new compounds contain one or two propylthio groups, which have been introduced in two ways. Direct reaction of arenediazonium salts with 1-propanethiolate gives yields comparable to those obtained in a three-step method through sulfonyl chlorides. The 1H- and 13C NMR chemical shifts of 17 1,2,3-trisubstituted benzenes have been correlated with the predicted values and the observed trends explained using commonly available modeling packages.
- Sienkowska, Monika,Benin, Vladimir,Kaszynski, Piotr
-
p. 165 - 173
(2007/10/03)
-
- 7-Substituted Benzothiophenes and 1,2-Benzisothiazoles. Part 2. Chloro and Nitro Derivatives
-
The 7-chloro and 7-nitro derivatives of benzothiophene and 1,2-benzisothiazole have been prepared from readily available precursors, which for each substituent are common to both ring systems. 7-Chlorobenzothiophene has been obtained from 3-chloro-2-mercaptobenzoic acid via 7-chlorobenzothiophen-3(2H)-one, or from 2,3-dichlorobenzaldehyde, either via β-(2,3-dichlorophenyl)-α-mercaptoacrylic acid (16) or, preferably, via 7-chlorobenzothiophene-2-carboxylic acid.Hexamethylphosphoric triamide is a particularly useful solvent in which to effect the selective nucleophilic replacement of the 2-chloro substituent in 2,3-dichlorobenzaldehyde. 7-Chloro-1,2-benzisothiazole is available by treatment of 3-chloro-2-mercaptobenzaldehyde with chloramine (57percent), or by heating 2,3-dichlorobenzaldehyde with sulphur and aqueous ammonia (46percent). 7-Nitrobenzothiophene has been obtained by treatment of 2-bromo-3-nitrobenzaldehyde with mercaptoacetic acid under alkaline conditions, followed by decarboxylation of the resulting 2-carboxylic acid.Cyclisation of 2-(n- or t-butylthio)-3-nitrobenzaldoxime with polyphosphoric acid gives 7-nitro-1,2-benzisothiazole in high yield. 3-Nitro-2-t-bytylthiobenzaldehyde behaves unexpectedly with chloramine, to give what is believed to be 7-nitro-2-t-butyl-1,2-benzothiazolium chloride (24) (73percent).
- Rahman, Loay K. A.,Scrowston, Richard M.
-
p. 385 - 390
(2007/10/02)
-