151378-81-3Relevant academic research and scientific papers
C-terminal 1-aminoethyltetrazole-containing oligopeptides as novel alanine racemase inhibitors
Anderson, Rosaleen J.,Gray, Mark,Kondacs, Laszlo A.,Marrs, Emma C. L.,Orenga, Sylvain,Perry, John D.
, (2020/03/19)
In clinical culture media inoculated with patient samples, selective inhibition of commensal bacteria is essential for accurate diagnosis and effective treatment, as they can mask the presence of pathogenic bacteria. The alanine analogue, 1-aminoethyltetr
Amidation of carboxylic acids via the mixed carbonic carboxylic anhydrides and its application to synthesis of antidepressant (1S,2R)-tranylcypromine
Ezawa, Tetsuya,Kawashima, Yuya,Noguchi, Takuya,Jung, Seunghee,Imai, Nobuyuki
, p. 1690 - 1699 (2017/11/14)
Primary amidations of carboxylic acids 1 or 3 with NH4Cl in the presence of ClCO2Et and Et3N were developed to afford the corresponding primary amides in 22% to quantitative yields. Additionally, we have applied the amidation to the preparation of various amides containing hydroxamic acids and achieved the synthesis of (1S,2R)-tranylcypromine as an antidepressant medicine via Lossen rearrangement.
Convenient preparation of primary amides via activation of carboxylic acids with ethyl chloroformate and triethylamine under mild conditions
Noguchi, Takuya,Sekine, Masahiro,Yokoo, Yuki,Jung, Seunghee,Imai, Nobuyuki
, p. 580 - 582 (2013/07/05)
Primary amides were easily prepared in 22-99% yields from the corresponding carboxylic acids 1 or 5 with NH4Cl via activation with ClCO 2Et and Et3N. The enantiomers of the corresponding primary amides of Cbz-, Boc-, or Fmoc-α-amino acids can be separated by using a chiral column.
Diacyl derivatives of propylene diamine having herbicidal activity
-
, (2008/06/13)
Novel herbicidal compounds are provided having the formula (I) wherein one of R1a and R1b is a methyl, hydroxymethyl or monohalomethyl group and the other is hydrogen; R2 is a group R3—(X1)m/sub
Design and synthesis of cyclopenta[g]quinazoline-based antifolates as inhibitors of thymidylate synthase and potential antitumor agents
Bavetsias, Vassilios,Marriott, Jonathan H.,Melin, Camille,Kimbell, Rosemary,Matusiak, Zbigniew S.,Boyle, F. Thomas,Jackman, Ann L.
, p. 1910 - 1926 (2007/10/03)
Following the development of raltitrexed, the synthesis of nonpolyglutamatable inhibitors of TS that do not use the reduced folate carrier (RFC) for cellular entry should provide compounds which overcome mechanisms of resistance to folate-based inhibitors
Carboxylic acid bioisosteres of γ-linked dipeptide analogues of the folate-based thymidylate synthase (TS) inhibitor, 2-desamino-2-methyl-N10-propargyl-5,8-dideazafolic acid (ICI 198583)
Bavetsias,Jackman,Kimbell,Boyle,Bisset
, p. 631 - 636 (2007/10/03)
Tetrazole carboxylic acid bioisosteres of γ-linked dipeptide derivatives of 2-desamino-2-methyl-N10-propargyl-5,8-dideazafolic acid (ICI 198583), a folate-based inhibitor of thymidylate synthase (TS), were synthesised by multistep routes starti
Enzymatic ammoniolysis of amino acid derivatives
Zoete, M. C. de,Ouwehand, A. A.,Rantwijk, F. van,Sheldon, R. A.
, p. 171 - 174 (2007/10/02)
The ammoniolysis of amino acid esters and their derivatives was performed with lipases and proteases yielding the corresponding amino acid amides with moderate to high enantioselectivity.Phenylglycine methyl ester racemized slowly under the reaction conditions.
