4254-31-3Relevant articles and documents
Scalable green approach toward fragrant acetates
Puchl'Ová, Eva,Szolcsányi, Peter
, (2020/08/07)
The advantageous properties of ethylene glycol diacetate (EGDA) qualify it as a useful substitute for glycerol triacetate (GTA) for various green applications. We scrutinised the lipase-mediated acetylation of structurally diverse alcohols in neat EGDA furnishing the range of naturally occurring fragrant acetates. We found that such enzymatic system exhibits high reactivity and selectivity towards activated (homo) allylic and non-activated primary/secondary alcohols. This feature was utilised in the scalable multigram synthesis of fragrant (Z)-hex-3-en-1-yl acetate in 70percent yield. In addition, the Lipozyme 435/EGDA system was also found to be applicable for the chemo-selective acetylation of (hydroxyalkyl) phenols as well as for the kinetic resolution of chiral secondary alcohols. Lastly, its discrimination power was demonstrated in competitive experiments of equimolar mixtures of two isomeric alcohols. This enabled the practical synthesis of 1-pentyl acetate isolated as a single product in 68percent yield from the equimolar mixture of 1-pentanol and 3-pentanol.
Method for preparing 5,6-diethyl-2,3-dihydro-1H-indene-2-amino hydrochloride
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Paragraph 0025; 0028; 0029, (2019/10/01)
The invention relates to a novel synthesis route of a method for preparing 5,6-diethyl-2,3-dihydro-1H-indene-2-amino hydrochloride. 2-indanol is adopted as a raw material, and 5,6-diethyl-2,3-dihydro-1H-indene-2-amino hydrochloride is synthesized with a high yield through seven steps of an acetylation reaction, a substitution reaction, a coupling reaction, a hydroxyl protection reaction, a substitution reaction, a reduction reaction and a salting reaction. The preparation method of the 5,6-diethyl-2,3-dihydro-1H-indene-2-amino hydrochloride, which is provided by the invention, is a preparationmethod which is high in yield, low in cost, friendly to the environment, easy to operate and applicable to industrialization.
ARYLPROPIONAMIDE, ARYLACRYLAMIDE, ARYLPROPYNAMIDE, OR ARYLMETHYLUREA ANALOGS AS FACTOR XIA INHIBITORS
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Page/Page column 220, (2008/06/13)
The present invention provides compounds of Formula (I): Formula (I) or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L1, M and R11 are as defined herein. The compounds of Formula (I) are selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.