77539-18-5Relevant articles and documents
Substituted 5-oxo-pyrrolidine derivative, and preparation method and applications thereof
-
Paragraph 0056-0057, (2019/01/21)
The invention belongs to the technical field of medicine, relates to a substituted 5-oxo-pyrrolidine derivative disclosed in generation formula I, and a preparation method and applications thereof, and more specifically relates to applications of the substituted 5-oxo-pyrrolidine derivative in preparation of anti-cerebral ischemia medicines as a nerve protective agent, and a pharmaceutical composition taking the substituted 5-oxo-pyrrolidine derivative and a pharmaceutically acceptable salt of the substituted 5-oxo-pyrrolidine derivative as active components. The pharmaceutical composition contains the substituted 5-oxo-pyrrolidine derivative and a pharmaceutical excipient and/or a diluent of the substituted 5-oxo-pyrrolidine derivative. In the general formula I, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, X, Y, and n are defined in the patent specification and patent claims.
A the non-peptide class perishes weakly inhibiting protein antagonists and its synthetic method and application (by machine translation)
-
Paragraph 0048; 0049; 0050; 0051, (2016/10/08)
This invention discloses a kind of the non-peptide class perishes weakly inhibiting protein antagonist and method for preparing the same and application, which aims to provide a better anticancer effect with the non-peptide class perishes weakly inhibitin
An efficient and straight forward strategy for the synthesis of enantiomerically pure (S)-1-benzyl-5-(alkyl/aryl amino) methyl-pyrrolidin-2-ones
Panday, Sharad Kumar,Pathak, Manoher Bhushan,Prasad, Jagdish
, p. 936 - 939 (2015/08/06)
A simple, efficient and straightforward strategy for the synthesis of enantiomerically pure (S)-5-((alkyl/aryl amino) methyl)-pyrrolidin-2-ones from N-benzyl-5(S)-pyroglutaminol through Mitsunobu reaction has been described. These pyrrolidin-2-ones have great potential to act as asymmetric precursors for the synthesis of bioactive compounds/ natural products requiring suitably substituted aminomethyl group at C-5 of native pyrrolidin-2-ones.
Electrophilic Amination of Amino Acids with N-Boc-oxaziridines: Efficient Preparation of N-Orthogonally Diprotected Hydrazino Acids and Piperazic Acid Derivatives
Hannachi, Jean-Christophe,Vidal, Joelle,Mulatier, Jean-Christophe,Collet, Andre
, p. 2367 - 2373 (2007/10/03)
A general two-step preparation of enantiopure Nα,N β-orthogonally diprotected α-hydrazino acids 1 is developed on a multigram scale. The key reaction is the efficient electrophilic amination of N-benzyl amino acids 6 with N-Boc-oxaziridine 7 and accommodates various functional groups encountered in side chains of amino acids. The cyclic 2,3,4,5-tetrahydro-3-pyridazine carboxylic acid (piperazic acid) derivatives 2 and 3 or the cyclic 3,4-dihydro-3-pyrazolecarboxylate 4 are conveniently prepared from glutamic acid or aspartic acid via orthogonally diprotected α-hydrazino acids 1m and 1n.
The first highly enantioselective homogeneously catalyzed asymmetric reductive amination: Synthesis of α-N-benzylamino acids
Kadyrov, Renat,Riermeier, Thomas H.,Dingerdissen, Uwe,Tararov, Vitali,Boerner, Armin
, p. 4067 - 4070 (2007/10/03)
High-throughput screening considering a library of 96 chiral P-ligands involved in two types of RhI complexes was used for the identification of homogeneous catalysts for the highly enantioselective reductive amination of α-keto acids with benzylamine. After optimization of the reaction conditions and scale-up with a cationic Rh-Deguphos catalyst, a range of chiral α-amino acids could be produced by this new reaction in good yield and by up to 98% ee.
Sodium borohydride: A versatile reagent in the reductive N-monoalkylation of α-amino acids and α-amino methyl esters
Verardo, Giancarlo,Geatti, Paola,Pol, Elena,Giumanini, Angelo G.
, p. 779 - 788 (2007/10/03)
α-Amino acids and α-amino methyl esters are easily converted to their N-monoalkyl derivatives by a reductive condensation reaction using several carbonyl compounds in the presence of sodium borohydride. This reducing agent has shown a wide versatility with minor but essential procedural variations. The reaction allows the α-monodeuterium labeling of the new N-substituent by use of sodium borodeuteride.
The improved synthesis of enantiopure (s)-N-arylmethyl-5-oxoprolines
Marchalin, Stefan,Kadlecikova, Katarina,Bar, Nathalie,Decroix, Bernard
, p. 3619 - 3624 (2007/10/03)
A mild procedure for the preparation of enantiopure N-alkylated (S)- (+)-5-oxoprolines 3a-r is described. The method starting from (S)-glutamic acid appears generally applicable to substrates with a wide range of substituents.
Peptide Mimetics of Thyrotropin-Releasing Hormone Based on a Cyclohexane Framework: Design, Synthesis, and Cognition-Enhancing Properties
Olson, Gary L.,Cheung, Ho-Chuen,Chiang, Elliot,Madison, Vincent S.,Sepinwall, Jerry,et al.
, p. 2866 - 2879 (2007/10/02)
The design and synthesis of peptide mimetics of thyrotropin-releasing hormone (TRH) in which the peptide backbone is entirely replaced by a cyclohexane framework are described.The cis-1,3,5-trisubstituted ring was expected to permit key pharmacophoric gro
NEW STRATEGY FOR THE CONSTRUCTION OF CARBAPENEMS. TOTAL SYNTHESIS OF 6-epi PS-5 AND PS-5
Koskinen, Ari M. P.,Ghiaci, Mehran
, p. 3209 - 3212 (2007/10/02)
A strategically novel approach to carbapenems has been developed.The pyrrolidine ring is first constructed, appended with the required side chains, and the β-lactam ring is then annealed.We have demonstrated the utility of the approach to the asymmetric s
AN EFFICIENT ONE-STEP REDUCTIVE N-MONOALKYLATION OF α-AMINO ACIDS
Ohfune, Yasufumi,Kurokawa, Natsuko,Higuchi, Naoki,Saito, Masayuki,Hashimoto, Masaki,et al.
, p. 441 - 444 (2007/10/02)
Reactions of protection-free α-amino acids with aldehydes or ketones in the presence of sodium cyanoborohydride afforded the N-monoalkylated amino acids in inorganic salt-free form.Application of this method to synthesis of N-alkyl derivatives of biologic