121885-10-7Relevant articles and documents
Homogeneous catalytic aminocarbonylation of nitrogen-containing iodo-heteroaromatics. Synthesis of N-substituted nicotinamide related compounds
Takács, Attila,Jakab, Balázs,Petz, Andrea,Kollár, László
, p. 10372 - 10378 (2008/02/13)
Various primary and secondary amines, including amino acid methyl esters, were used as nucleophiles in palladium-catalysed aminocarbonylation of 2-iodopyridine, 3-iodopyridine and iodopyrazine. N-Substituted nicotinamides and 3-pyridyl-glyoxylamides (2-oxo-carboxamide type derivatives) of potential biological importance can be obtained from 3-iodopyridine as a result of simple and double carbon monoxide insertions, respectively. The latter examples can be obtained in synthetically acceptable yields by using elevated carbon monoxide pressure. On the contrary, N-alkyl/aryl-carboxamides were obtained exclusively in the whole pressure range by using 2-iodopyridine and iodopyrazine.
Amide derivative
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, (2008/06/13)
A compound of the formula: wherein Ar is optionally substituted phenyl, etc.; n is 0, 1 or 2; R1is hydogen atom, optionally substituted alkyl, etc.; R2and R3are independently optionally substituted alkyl, etc.; R4and R5are independently hydrogen atom or optionally substituted alkyl; R6is hydrogen atom, hydroxy or alkyl; or a pharmaceutically acceptable salt thereof is useful as a medicament for treating retinal degenerative disorders and the like.
N-acylbenzotriazoles: Neutral acylating reagents for the preparation of primary, secondary, and tertiary amides
Katritzky,He,Suzuki
, p. 8210 - 8213 (2007/10/03)
Readily available N-acylbenzotriazoles 2a-q efficiently acylate aqueous ammonia and primary and secondary amines to give primary, secondary, and tertiary amides in good to excellent yields. The wide applicability of the procedure is illustrated by the preparation of (i) α-hydroxyamides from α-hydroxy acids and of (ii) perfluoroalkylated amides.
Process for the preparation of optically active piperazine-2-carboxylic acid derivatives
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, (2008/06/13)
Optically active piperazine-2-carboxylic acid derivatives of the general formula: STR1 in which X is alkoxy or a (substituted) amino group, are prepared by asymmetric hydrogenation of the corresponding pyrazinecarboxylic acid derivatives, catalyzed by optically active rhodium complexes. The compounds of the formula I are intermediates for the preparation of pharmaceutical active substances, for example, HIV protease inhibitors.
Process for preparing N-tert-butyl-2-pyrazinecarboxamide and N-tert-butyl-2-piperazinecarboxamide
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, (2008/06/13)
A process for preparing a N-tert-butyl-2-pyrazinecarboxamide having the formula (2): STR1 which comprises reacting a cyanopyrazine having the formula (1): STR2 with tert-butyl alcohol in the presence of sulfuric acid and a process for preparing a N-tert-butyl-2-piperazine-carboxamide having the formula (3): STR3 which comprises hydrogenating of said N-tert-butyl-2-pyrazinecarboxamide having the formula (2) in the presence of Raney nickel or Raney cobalt.
Highly Diastereoselective Reaction of a Chiral, Non-Racemic Amide Enolate with (S)-Glycidyl Tosylate. Synthesis of the Orally Active HIV-1 Protease Inhibitor L-735,524
Askin, David,Eng, Kan K.,Rossen, Kai,Purick, Robert M.,Wells, Kenneth M.,et al.
, p. 673 - 676 (2007/10/02)
Reaction of chiral amide enolate Li-1 with (S)-glycidyl tosylate 11 affords the epoxide 3 in 72percent yield with high diastereoselectivity.Epoxide 3 is converted to the orally-active HIV-1 protease inhibitor L-735,524 in 71percent isolated yield.