81699-67-4Relevant articles and documents
Mapping the mechanism of nickel-ferrophite catalysed methylation of baylis-hillman-derived SN2′ electrophiles
Novak, Andrew,Calhorda, Maria Jose,Costa, Paulo Jorge,Woodward, Simon
experimental part, p. 898 - 903 (2009/07/19)
Enantioselective Ni-catalysed methylation of Baylis-Hillman-derived allylic electrophiles in the presence of ferrophite ligands has been investigated computationally and experimentally. The sense and degree of enantioselectivity attained is independent of both the leaving group and the isomeric structure of the initial allylic halide. DFT studies support the selective formation of a limited number of energetically favoured anti and syn π-allyl intermediates. The observed regio- and enantioselectivity can be rationalised based on the energetics of these structures.
Toward an optimal joint recognition of the s1′ subsites of endothelin converting enzyme-1 (ECE-1), angiotensin converting enzyme (ACE), and neutral endopeptidase (NEP)
Inguimbert, Nicolas,Coric, Pascale,Poras, Hervé,Meudal, Hervé,Teffot, Franck,Fournié-Zaluski, Marie-Claude,Roques, Bernard P.
, p. 1477 - 1486 (2007/10/03)
The formation of vasoconstrictors (e.g., angiotensin II and endothelin) and the inactivation of vasodilators (e.g., bradykinin and atrial natriuretic) by membrane-bound zinc metallopeptidases are key mechanisms in the control of blood pressure and fluid h
N-[MERCAPTOACYL(AMINO ACID OR PEPTIDE)] COMPOUNDS AND S-LIPOPHILIC ALIPHATIC CARBONYL DERIVATIVES THEREOF AS ANTIHYPERTENSIVES
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, (2008/06/13)
N-[Mercaptoacyl(amino acid or peptide)] compounds and S-lipophilic aliphatic carbonyl derivatives thereof, and pharmaceutical compositions comprising such compounds, as well as the use of these compounds as antihypertensives by the inhibition of neutral endopeptidase and/or peptidyldipeptidase A are disclosed. Methods for preparing the such compounds and derivatives are disclosed also.
New dual inhibitors of neutral endopeptidase and angiotensin-converting enzyme: Rational design, bioavailability, and pharmacological responses in experimental hypertension
Fournie-Zaluski,Coric,Turcaud,Rousselet,Gonzalez,Barbe,Pham,Jullian,Michel,Roques
, p. 1070 - 1083 (2007/10/02)
In the treatment of cardiovascular diseases, it could be of therapeutic interest to associate the hypotensive effects resulting from the inhibition of angiotensin II formation, ensured by endothelial angiotensin-converting enzyme (ACE), with the diuretic
N-(mercaptoacyl)amino acids, methods of their preparation and therapeutic use, and pharmaceutical compositions containing them
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, (2008/06/13)
The present invention is directed to a compound of the formula (I) wherein, R represents a hydrogen atom or an acyl, aroyl or cycloalkylcarbonyl radical or a residue of formula R1 represents an alkyl radical;, R2 represents an aryl o
A NOVEL ROUTE TO SUBSTITUTED PHOSPHONATES VIA CONJUGATE ADDITION OF ORGANOMETALLICS TO 1-(FUNCTIONALLY) SUBSTITUTED ALKENE PHOSPHONATES.
Barbot, F.,Paraiso, E.,Miginac, Ph.
, p. 4369 - 4370 (2007/10/02)
Organometallics readily add to the double bond of 1-(functionally) substituted alkene phosphonates to give highly substituted phosphonates.
AN INTERPRETATION OF THE SUBSTITUENT EFFECT IN THE BLAISE REARRANGEMENT IN TERMS OF PI-ORBITALS
Abe, Yukio,Suehiro, Tadashi
, p. 389 - 392 (2007/10/02)
The migratory aptitude of the substituent groups in the Blaise rearrangement can be explained in terms of the pi-electronic properties of the groups in the highest occupied molecular orbitals.The rates of the rearrangement reaction with relation to the substituent groups were also rationally understood based on the energy levels of the molecular orbitals.
FORMATION OF CYCLOPROPANE DERIVATIVES IN THE BLAISE REARRANGEMENT
Abe, Yukio,Suehiro, Tadashi
, p. 337 - 340 (2007/10/02)
On heating tosylates of ethyl 2-alkyl-2-methyl-3-hydroxy-3-phenylpropanoate (R=Me, 1b; R=Et, 6) in o-dichlorobenzene at 170 deg C, ethyl 1- methyl-2-phenyl- and 1,2-dimethyl-3-phenylcyclopropanecarboxylates, 3, and 8, were formed in both 5percent yield, respectively, whereas the alkyl migration products, ethyl 3-alkyl-2-methyl-3-phenylpropenoates, were not produced.The mode of the reaction of the methyl group with the cationic carbon was described.
