- Sustainable organophosphorus-catalysed Staudinger reduction
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A highly efficient and sustainable catalytic Staudinger reduction for the conversion of organic azides to amines in excellent yields has been developed. The reaction displays excellent functional group tolerance to functionalities that are otherwise prone to reduction, such as sulfones, esters, amides, ketones, nitriles, alkenes, and benzyl ethers. The green nature of the reaction is exemplified by the use of PMHS, CPME, and a lack of column chromatography.
- Lenstra, Danny C.,Lenting, Peter E.,Mecinovi?, Jasmin
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p. 4418 - 4422
(2018/10/17)
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- Regio- and stereoselective hydroamination of alkynes using an ammonia surrogate: Synthesis of N -Silylenamines as reactive synthons
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An anti-Markovnikov selective hydroamination of alkynes with N-silylamines to afford N-silylenamines is reported. The reaction is catalyzed by a bis(amidate)bis(amido)Ti(IV) catalyst and is compatible with a variety of terminal and internal alkynes. Stoichiometric mechanistic studies were also performed. This method easily affords interesting N-silylenamine synthons in good to excellent yields and the easily removable silyl protecting group enables the catalytic synthesis of primary amines.
- Lui, Erica K. J.,Brandt, Jason W.,Schafer, Laurel L.
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supporting information
p. 4973 - 4976
(2018/04/24)
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- ANTIULCER BENZIMIDAZOLE DERIVATIVES
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Compounds of formula I STR1 in which R 1 and R 2, which may be the same or different, are hydrogen, a C 1 to C 3 alkyl group or R 1 and R 2 together with the nitrogen to which they are attached form an optionally substituted heterocyclic ring; R 3 and R. sub.4, which may be the same or different are hydrogen, a C 1 to C. sub.3 alkyl or an optionally substituted C 3 to C 6 cycloalkyl group, or R 3 and R 4 together with the nitrogen to which they are attached form an optionally substituted heterocyclic ring; m is 0, 1 or 2; p is 0, 1 or 2; E is an alkylene group connected to or interrupted by an oxygen or a sulphur atom; J is hydrogen or a substituent group; and their pharmaceutically acceptable salts have utility as histamine H 2-receptor antagonists.
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