123724-21-0Relevant articles and documents
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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Paragraph 0459; 0460, (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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Paragraph 0163-0164, (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
HIV PROTEASE INHIBITORS, COMPOSITIONS CONTAINING THE SAME AND THEIR PHARMACEUTICAL USES
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Page/Page column 110, (2010/02/11)
This invention relates to a novel series of chemical compounds useful as Human immunodeficiency Virus (HIV) protease inhibitors and to the use of such compounds as antiviral agents. The invention further relates to pharmaceutical compositions containing s
Virtually complete control of simple and face diastereoselectivity in the Michael addition reactions between achiral equivalents of a nucleophilic glycine and (S)- or (R)-3-(E-enoyl)-4-phenyl-1,3-oxazolidin-2-ones: Practical method for preparation of β-substituted pyroglutamic acids and prolines
Soloshonok, Vadim A.,Ueki, Hisanori,Tiwari, Rohit,Cai, Chaozhong,Hruby, Victor J.
, p. 4984 - 4990 (2007/10/03)
This study demonstrates a new strategy for controlling the stereochemical outcome of the Michael addition reactions between nucleophilic glycine equivalents and α,β-unsaturated carboxylic acid derivatives: The addition reactions between achiral Ni(II)-complex of the Schiff base of glycine with o-[N-α-pycolylamino]acetophenone and (S)- or (R)-3-(E-enoyl)-4- phenyl-1,3-oxazolidin-2-ones were shown to occur at room temperature in the presence of nonchelating organic bases and, most notably, with very high stereoselectivity at both newly formed stereogenic centers. Thus, the chiral 4-phenyl-1,3-oxazolidin-2-one moiety was found to control efficiently both face diastereoselectivities of the glycine derived enolate and the C,C double bond of the Michael acceptor. The new strategy developed in this work is methodologically superior to previous methods, most notably in terms of generality and synthetic efficiency. Excellent chemical yields and diastereoselectivities, combined with the simplicity of the experimental procedures, render the present method of immediate use for preparing various 3-substituted pyroglutamic acids and related amino acids (glutamic acids, glutamines, prolines, etc.) available via conventional transformations of the former.
Boronic ester and acid compounds, synthesis and uses
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, (2008/06/13)
Disclosed herein are boronic ester and acid compounds, their synthesis and uses. More specifically, disclosed herein is a method for reducing the rate of degradation of proteins in an animal comprising contacting cells of the animal with certain boronic ester and acid compounds.
BORONIC ESTER AND ACID COMPOUNDS
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, (2008/06/13)
Disclosed herein is a method for reducing the rate of degradation of proteins in an animal comprising contacting cells of the animal with certain boronic ester and acid compounds. Also disclosed herein are novel boronic ester and acid compounds, their synthesis and uses.
Synthesis of Homochiral 3-Substituted Glutamic Acids and Prolines from Pyroglutamic Acid
Herdeis, Claus,Hubmann, Hans Peter,Lotter, Hermann
, p. 351 - 354 (2007/10/02)
Efficient syntheses of (2S,3S)-methylproline (5a) and (2S,3R)-phenylproline (5b) are described, starting from the readily available pyroglutaminol derivatives 2a and 2b via conjugate 1,4=addition of organocuprates to 1.Catalytic hydrogenation of 3 from th