210420-48-7Relevant academic research and scientific papers
Intermediate used for synthesis of (2S, 3R)-3-substituted phenyl pyrrolidine-2-carboxylic acid, and preparation method and applications thereof
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Paragraph 0054; 0064-0065, (2019/12/08)
The invention relates to an intermediate used for synthesis of (2S, 3R)-3-substituted phenyl pyrrolidine-2-carboxylic acid, and a preparation method and applications thereof. The preparation method ismainly used for solving a technical problem that no app
CONDENSED 5-OXAZOLIDINONE DERIVATIVE
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, (2016/12/01)
Provided are condensed 5-oxazolidinone derivatives and pharmaceutically permissible salts thereof, which have excellent anticoagulant effects, are well absorbed orally, and are useful as therapeutic drugs for thrombosis, etc. Compounds represented by form
1-(CYCLOALKYL-CARBONYL)PROLINE DERIVATIVE
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, (2015/06/03)
A compound represented by formula (1) (in the formula: ring-D represents a three- to eight-membered hydrocarbon ring; Ra represents an optionally substituted amino C1-6 alkyl group or the like; Rb1 and Rb2 each independently represent a hydrogen atom, a halogen atom, or the like; Rc represents an optionally substituted C6-10 aryl group or the like; Rd represents a hydrogen atom or the like; and ring-Q represents a (hetero)aryl group or the like which may be substituted with a carboxyl group or the like) or a pharmaceutically acceptable salt thereof exhibits an excellent FXIa inhibitory activity, and is useful as a therapeutic agent against thrombosis or the like.
1-(HETEROARYL CARBONYL) PROLINE DERIVATIVE
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, (2016/10/10)
PROBLEM TO BE SOLVED: To provide a 3-substituted proline derivative having excellent FXIa inhibitory activity and useful as a therapeutic agent for thrombosis or the like, and its pharmaceutically acceptable salt. SOLUTION: This invention relates to a com
Access to enantiomerically pure cis- and trans-β-phenylproline by high-performance liquid chromatography resolution
Fatás, Paola,Gil, Ana M.,Calaza, M. Isabel,Jiménez, Ana I.,Cativiela, Carlos
, p. 1082 - 1091 (2013/02/22)
The preparation of all four stereoisomers of the proline analog that bears a phenyl group attached to the β carbon either cis or trans to the carboxylic acid (cis- and trans-β-phenylproline, respectively) has been addressed. The methodology developed allows access to multigram quantities of the target amino acids in enantiomerically pure form and suitably protected for use in peptide synthesis. Racemic precursors of cis-β-phenylproline and trans-β-phenylproline were prepared from easily available starting materials and subjected to high-performance liquid chromatography enantioseparation. Semipreparative columns (250 × 20 mm) containing chiral stationary phases based on amylose (Chiralpak IA) (Daicel-Chiral Technologies Europe, Illkirch, France) or cellulose (Chiralpak IC) were used respectively for the resolution of the cis- and trans-β-phenylproline precursors. Chirality, 24:1082-1091, 2012. 2012 Wiley Periodicals, Inc. Copyright
Asymmetric synthesis of proline-based conformationally constrained tryptophan mimetic
Delaye, Pierre-Olivier,Vasse, Jean-Luc,Szymoniak, Jan
supporting information; experimental part, p. 3635 - 3637 (2010/09/06)
The synthesis of an optically pure proline-based tryptophan mimetic is described. The strategy involves the in situ generation of an unprecedented allylmetal species containing the indole moiety, and its coupling with a chiral imine. The construction of the 3-substitued proline skeleton is then achieved through a hydrozirconation/iodination sequence applied to the resulting homoallylic amine.
Diphenylprolinol silyl ether as a catalyst in an asymmetric, catalytic, and direct michael reaction of nitroethanol with α,β-unsaturated aldehydes
Gotoh, Hlroaki,Okamura, Daichi,Lshikawa, Hayato,Hayashl, Yujlro
supporting information; experimental part, p. 4056 - 4059 (2009/12/06)
Diphenylprollnol silyl ether was found to be an effective organocatalyst in the enantioselective and direct Michael reaction of nitroethanol and α,β-unsaturated aldehydes, affording the 1-hydroxy-trans-3,4- disubstituted tetrahydropyrans after isomerizatl
Design and synthesis of 3-arylpyrrolidine-2-carboxamide derivatives as melanocortin-4 receptor ligands
Tran, Joe A.,Tucci, Fabio C.,Arellano, Melissa,Jiang, Wanlong,Chen, Caroline W.,Marinkovic, Dragan,Fleck, Beth A.,Wen, Jenny,Foster, Alan C.,Chen, Chen
, p. 1931 - 1938 (2008/09/20)
Based on 3-phenylpropionamides, a series of 3-arylpyrrolidine-2-carboxamide derivatives was designed and synthesized to study the effect of cyclizations as melanocortin-4 receptor ligands. It was found that the 2R,3R-pyrrolidine isomer possessed the most
PIPERIDINE AND PYRROLIDINE BETA-SECRETASE INHIBITORS FOR THE TREATMENT OF ALZHEIMER'S DISEASE
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Page/Page column 36, (2008/06/13)
The present invention is directed to compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
Organocatalytic asymmetric 5-hydroxypyrrolidine synthesis: a highly enantioselective route to 3-substituted proline derivatives
Rios, Ramon,Ibrahem, Ismail,Vesely, Jan,Sundén, Henrik,Córdova, Armando
, p. 8695 - 8699 (2008/03/14)
The highly enantioselective organocatalytic tandem reaction between 2-acylaminomalonates and α,β-unsaturated aldehydes is presented. The reaction is a direct entry to 5-hydroxypyrrolidines and 3-substituted proline derivatives, which are furnished in high
