865620-61-7Relevant academic research and scientific papers
Thiazole sulfonamide compounds for the treatment of neurodegenerative disorders
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Page/Page column 14, (2010/02/14)
The present invention relates to compounds of the Formula: wherein R1 to R6, X, Z and A are as defined. These compounds have activity inhibiting production of Aβ-peptide. The invention also relates to pharmaceutical compositions and
Ring closure reactions of disubstituted 4-penten-1-oxyl radicals - Towards a stereoselective synthesis of allo-muscarine
Hartung, Jens,Kneuer, Rainer
, p. 1677 - 1683 (2007/10/03)
The trisubstituted functionalized tetrahydrofurans 10, 11, 16, 18, and 19 were photochemically prepared from 2,3-syn- and 2,3-anti-configured N-(3- benzoyloxy-5-hexen-2-oxy)thiazole-2(3H)-thione anti-6, pyridinethiones 7, anti-8, and BrCCl3. The formation of tetrahydrofurans was achieved by an efficient and highly regioselective alkoxyl radical cyclization (5-exo-trig). The 2,3-anti substituted intermediates 9 and 12 cyclize stereoselectively whereas a 2,3-syn-configured O-radical affords both possible diastereomeric addition products in equal amounts. The cyclized tetrahydrofuryl methyl radicals were trapped with the bromine atom donor BrCCl3 to afford the bromomethyl-substituted cyclic ethers 10, 11, 18, and 19 in excellent yields. The utility of this reaction was stressed by conversion of one of the newly prepared tetrahydrofurans in a two-step synthesis into (+)-allo-muscarine (+)-20.
